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US4876248A
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Anti-inflammatory products derived from methylene-diphosphonic acid, and process for their preparation
Assignee: Sanofi Aventis France
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Filing: 1988-03-07
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Granted: 1989-10-24
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Expires: 2008-03-07
Abstract
Abstract The present invention relates to products of the formula <IMAGE> (I) where R1 is H or alkyl, n is an integer from 0 to 10, and R2 is chosen from amongst H, unsubstituted or substituted alkyl radicals, a <IMAGE> group, a substituted or unsubstituted phenyl radical, a <IMAGE> 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 R3 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).
Inventors
- 👤 Jean C. Breliere
- 👤 Xavier Emonds-Alt
- 👤 Georges Garcia
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 06:59
CPC Classifications
C; C07; C07F; C07F9/00; C07F9/02; C07F9/28; C07F9/38; C07F9/547; C07F9/6536; C07F9/6539; C07F9/6541; A; A61; A61P; A61P29/00; C07F9/3804; C07F9/3839; C07F9/3865; C07F9/40; C07F9/4003; C07F9/4025; C07F9/4043; C07F9/553; C07F9/576; C07F9/58; C07F9/645; C07F9/6503; C07F9/6506; C07F9/65068; C07F9/6509; C07F9/6512; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 7
Claim 1
Independent Claim
161 words
A methylene-diphosphonic acid compound having the formula: ##STR56## in which: R 1 is hydrogen or a straight or branched lower alkyl group having from 1 to 4 carbon atoms, R 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 2 group, a COOH group; R 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 3 is OH, and with the further proviso that: R 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 1 is a methyl or ethyl group, R 3 is hydrogen and n=0; and the salts of said compounds with inorganic or organic bases when R 1 =H.
Claim 2
Dependent Claim
161 words
A methylene-diphosphonic acid compound having the formula: ##STR56## in which: R 1 is hydrogen or a straight or branched lower alkyl group having from 1 to 4 carbon atoms, R 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 2 group, a COOH group; R 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 3 is OH, and with the further proviso that: R 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 1 is a methyl or ethyl group, R 3 is hydrogen and n=0; and the salts of said compounds with inorganic or organic bases when R 1 =H.
Claim 3
Dependent Claim
35 words
A methylene-disphosphonic acid compound according to claim 1, having the formula (I) in which n=0 and ##STR58## R 3 =H, and the salts of said compounds with inorganic or organic bases when R 1 =H.
Claim 4
Dependent Claim
22 words
A methylene-disphosphonic acid compound according to claim 1, having the formula: ##STR59## or one of its salts with inorganic or organic bases.
Claim 5
Dependent Claim
122 words
Pharmaceutical compositions which contain in association with a pharmaceutically acceptable carrier an effective amount of a compound of formula (I): ##STR60## in which: R 1 is hydrogen or a straight or branched lower alkyl group having from 1 to 4 carbon atoms R 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 2 group, a COOH group; R 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 3 is OH; or of one of its salts with inorganic or organic bases when R 1 =H.
Claim 6
Dependent Claim
122 words
Pharmaceutical compositions which contain in association with a pharmaceutically acceptable carrier an effective amount of a compound of formula (I): ##STR60## in which: R 1 is hydrogen or a straight or branched lower alkyl group having from 1 to 4 carbon atoms R 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 2 group, a COOH group; R 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 3 is OH; or of one of its salts with inorganic or organic bases when R 1 =H.
Claim 7
Dependent Claim
24 words
A pharmaceutical composition according to claim 4, which contains from 10 to 500 mg of the compound of formula I as an active ingredient.
References Cited (Backward Citations)
US3299123A
Cited
US3654151A
Cited
US3705191A
Cited
US3957858A
Cited
US3683080A
Cited
US4171373A
Cited
US4071584A
Cited
US4264582A
Cited
EP0015370A1
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-10-23 | 1993-04-24 | 1993-10-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-10-23 | 1997-04-24 | 1997-10-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-10-23 | 2001-04-24 | 2001-10-24 | $7700.00 | Window Closed / Lapsed |