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US4711880A Expired / Lapsed US ⏱️ 0.0 years remaining

Crystalline disodium 3-amino-1-hydroxypropane-1,1-diphosphonate pentahydrate

Assignee: Henkel AG and Co KGaA
•
Filing: 1986-09-08
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Granted: 1987-12-08
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Expires: 2006-09-08
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Abstract

Abstract The invention relates to a novel crystal modification, containing water of crystallization, of disodium 3-amino-1-hydroxypropane-1,1-diphosphonate of the formula <IMAGE> and to a process for the manufacture thereof. This modification is suitable for the oral treatment of disorders of the calcium and phosphate metabolism and associated diseases in warm-blooded animals.

Inventors

  • 👤 Peter H. Stahl
  • 👤 Beat Schmitz

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-06 12:05
CPC Classifications
C; C07; C07F; C07F9/00; C07F9/02; C07F9/06; C07F9/16; C07F9/165; C07F9/28; C07F9/38; C07F9/3804; C07F9/3839; C07F9/3873; A; A61; A61P; A61P3/00; A61P3/12; A61P3/14

Claims Analysis

Total Claims: 10
Claim 1
Independent Claim 15 words
Disodium 3-amino-1-hydroxypropane-1,1-diphosphonate of the formula ##STR3## in a crystalline form that contains water of crystallisation.
Claim 2
Dependent Claim 15 words
Disodium 3-amino-1-hydroxypropane-1,1-diphosphonate of the formula ##STR3## in a crystalline form that contains water of crystallisation.
Claim 3
Dependent Claim 29 words
Disodium 3-amino-1-hydroxypropane-1,1-diphosphonate in a crystalline form that contains water of crystallisation according to claim 1, characterised by a water content of from approximately 24.1 to approximately 24.5% by weight.
Claim 4
Dependent Claim 10 words
Disodium 3-amino-1-hydroxypropane-1,1-diphosphonate according to claim 1 in crystalline pentahydrate form.
Claim 5
Dependent Claim 24 words
Disodium 3-amino-1-hydroxypropane-1,1-diphosphonate according to claim 1, obtainable by crystallisation of disodium 3-amino-1-hydroxypropane-1,1-diphosphonate from a water-containing solution and drying at normal or slightly elevated temperature.
Claim 6
Dependent Claim 37 words
Disodium 3-amino-1-hydroxypropane-1,1-diphosphonate according to claim 1, obtainable by crystallisation from an at least saturated aqueous solution, crystal formation taking place at at least approximately 50° C., and drying at from approximately 15° C. to approximately 60° C.
Claim 7
Dependent Claim 50 words
Disodium 3-amino-1-hydroxypropane-1,1-diphosphonate according to claim 1, obtainable by crystallisation from an at least saturated aqueous solution, crystal formation taking place at from approximately 50° C. to approximately 80° C., and drying at from approximately 18° C. to approximately 25° C. or at from approximately 35° C. to approximately 40° C.
Claim 8
Dependent Claim 34 words
Disodium 3-amino-1-hydroxypropane-1,1-diphosphonate according to claim 1, obtainable by the action of moist air having a relative atmospheric humidity of from approximately 95% to approximately 99% at from approximately 20° C. to approximately 25° C.
Claim 9
Dependent Claim 152 words
Disodium 3-amino-1-hydroxypropane-1,1-diphosphonate in a crystalline form that contains water of crystallisation according to claim 1, characterised by the following lattice spacings (d-values) and relative line intensities (intensities) of its X-ray powder pattern (camera according to Guinier-de-Wolff, radiation source: copper-K.sub.α): ______________________________________ d-values (Ångstrom) Intensities ______________________________________ 10.2 medium 9.9 medium 9.2 very strong 5.91 very strong 5.57 strong 5.42 very weak 5.30 strong 5.14 medium 5.02 very strong 4.97 very strong 4.63 very weak 4.41 strong 4.16 strong 4.07 weak 4.04 medium 3.95 very weak 3.75 strong 3.67 weak 3.63 medium 3.61 very weak 3.58 very weak 3.51 medium 3.43 strong 3.38 medium 3.15 medium 3.14 medium 3.09 medium 3.03 very strong 3.01 very strong 2.98 strong 2.97 very weak 2.91 very strong 2.82 strong 2.80 medium 2.78 medium 2.75 strong 2.73 weak 2.71 weak 2.69 weak 2.67 medium 2.66 medium 2.63 strong 2.62 strong 2.61 strong 2.58 very strong 2.57 very strong ______________________________________
Claim 10
Dependent Claim 40 words
Pharmaceutical preparations intended for enteral administration to warm-blooded animals, containing disodium 3-amino-1-hydroxypropane-1,1-diphosphonate in addition to customary pharmaceutical auxiliaries, characterised in that they contain the mentioned active ingredient in a crystalline form that contains water of crystallisation according to claim 1.

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USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1990-12-07 1991-06-08 1991-12-08 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1994-12-07 1995-06-08 1995-12-08 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1998-12-07 1999-06-08 1999-12-08 $7700.00 Window Closed / Lapsed

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