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Pharmacologically active biphosphonates, process for the preparation thereof and pharmaceutical compositions therefrom

Assignee: Merck and Co Inc
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Filing: 1984-06-08
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Granted: 1986-11-04
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Expires: 2004-06-08
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Abstract

Abstract Biphosphonic acids of general formula I: <IMAGE> (I) in which R is a fluorine atom of a linear or branched alkyl radical containing between 1 and 5 carbon atoms, which may also be substituted by one or more amino groups of fluorine atoms or both amino groups and fluorine atoms, R' is hydroxy or fluorine, and their salts with an alkali metal, an organic base or a basic aminoacid, exhibit valuable properties in the treatment of urolithiasis or in the treatment as inhibitors of bone reabsorption. The compound 4-amino-1-hydroxybutan-1,1-biphosphonic acid is between 100 and 300 times more active than Cl2MDP.

Inventors

  • 👤 Sergio Rosini
  • 👤 Giorgio Staibano

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-08 11:16
CPC Classifications
C; C07; C07F; C07F9/00; C07F9/02; C07F9/28; C07F9/38; C07F9/3804; C07F9/3839; C07F9/3873; A; A61; A61P; A61P13/00; A61P13/02; A61P15/00; A61P3/00; C07F9/3856

Claims Analysis

Total Claims: 2
Claim 1
Independent Claim 26 words
A method of treatment of urolithiasis and inhibiting bone reabsorption which consists of administering to a patient in need thereof an effective amount of 4-amino-1-hydroxybutane-1,1-biphosphonic acid.
Claim 2
Independent Claim 26 words
A method of treatment of urolithiasis and inhibiting bone reabsorption which consists of administering to a patient in need thereof an effective amount of 4-amino-1-hydroxybutane-1,1-biphosphonic acid.

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1989-11-03 1990-05-05 1990-11-04 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1993-11-03 1994-05-05 1994-11-04 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1997-11-03 1998-05-05 1998-11-04 $7700.00 Window Closed / Lapsed

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