114084-78-5 Usage
Description
This third generation biphosphonate was launched in Austria and Germany
for the treatment of bone disorders such as hypercalcemia in malignancy and
ostedysis, Paget's disease and osteoporosis. It does not effect bone mineralization,
therefore, the potential risk of osteomalacia is prevented. This was a problem with
first generation derivatives. While the exact mode of action is not understood, they
are inhibitors of osteroclast mediated bone resorption. These compounds strongly
interact with hydroxyapatite crystals and have a half-life in the skeleton of several
years. Despite this observation ibandronate was well tolerated and safe.
Chemical Properties
White Solid
Originator
Boehringer Mannheim (Germany)
Uses
Different sources of media describe the Uses of 114084-78-5 differently. You can refer to the following data:
1. A biphosphonate bone resorption inhibitor.
2. A labeled biphosphonate bone resorption inhibitor.
3. A bisphosphonate antiresorptive agent. Bone resorption inhibitor.
4. Labelled Ibandronic Acid (I120000). A bisphosphonate antiresorptive agent. Bone resorption inhibitor.
Brand name
Bondronat
Clinical Use
Bisphosphonate:
Reduction of bone damage in bone metastases in
breast cancer
Hypercalcaemia of malignancy
Postmenopausal osteoporosis
Drug interactions
Potentially hazardous interactions with other drugs
None known
Metabolism
After initial systemic exposure, ibandronic acid rapidly
binds to bone or is excreted into urine. There is no
evidence that ibandronic acid is metabolised in animals
or humans. The absorbed fraction of ibandronic acid
is removed from the circulation via bone absorption
(estimated to be 40-50% in postmenopausal women)
and the remainder is eliminated unchanged by the kidney.
The unabsorbed fraction of ibandronic acid is eliminated
unchanged in the faeces. Renal clearance accounts for
50-60% of total clearance and is related to creatinine
clearance. The difference between the apparent total and
renal clearances is considered to reflect the uptake by
bone.
Check Digit Verification of cas no
The CAS Registry Mumber 114084-78-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,1,4,0,8 and 4 respectively; the second part has 2 digits, 7 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 114084-78:
(8*1)+(7*1)+(6*4)+(5*0)+(4*8)+(3*4)+(2*7)+(1*8)=105
105 % 10 = 5
So 114084-78-5 is a valid CAS Registry Number.
InChI:InChI=1/C9H23NO7P2/c1-3-4-5-7-10(2)8-6-9(11,18(12,13)14)19(15,16)17/h11H,3-8H2,1-2H3,(H2,12,13,14)(H2,15,16,17)
114084-78-5Relevant articles and documents
Rational synthesis of α-hydroxyphosphonic derivatives including dronic acids
Grün, Alajos,Rádai, Zita,S?regi-Nagy, Dávid Illés,Greiner, István,Keglevich, Gy?rgy
, p. 386 - 387 (2019/01/18)
New, green methods have been elaborated for the syntheses of α-hydroxyphosphonates and α-hydroxymethylenebisphosphonic derivatives (HMBPs, dronates). α-Hydroxyphosphonates were prepared via the Pudovik reaction, while the synthesis of HMBPs has been performed in the three-component reaction of carboxylic acids, phosphorus trichloride and phosphorus acid.
Preparation of ibandronate trisodium
-
Page/Page column 5, (2010/05/13)
The trisodium salt of ibandronate of formula (I): A process of preparing said salt comprises: a) mixing 3-(methylpentylamino)propionic acid hydrochloride, phosphorous acid (in a 2.5-3.5 molar excess with respect to 3-(methylpentylamino)propionic acid hydrochloride), sunflower oil (in an amount of 6-9 volume parts for 1 weight part of 3-(methylpentylamino)propionic acid hydrochloride) and phosphorus trichloride (in a 3-4 molar excess with respect to 3-(methylpentylamino)propionic acid hydrochloride); b) adding water (in an amount of 6-9 volume parts for 1 weight part of 3-(methylpentylamino)propionic acid hydrochloride) and after separation of the phases; c) adjusting pH of the water phase to pH 12.5; d) adding a water-miscible co-solvent and cooling down to precipitate the product or evaporate to dryness. Another process for preparing the trisodium salt of ibandronate comprises admixing the monosodium salt of ibandronate or ibandronic acid or their solvates with water or a mixture water/sodium hydroxide and adjustment of pH to 12.5. Various crystalline, semicrystalline and amorphous forms of trisodium ibandronate are disclosed.
CRYSTALLINE FORM A OF IBANDRONIC ACID AND PROCESS FOR THE PREPARATION
-
Page/Page column 23-24, (2008/06/13)
The present invention relates crystalline Form A of Ibandronic acid having Formula (I) and a process for the preparation thereof.
