76541-76-9Relevant academic research and scientific papers
Copper-mediated 1,4-conjugate addition of boronic acids and indoles to vinylidenebisphosphonate leading to gem-bisphosphonates as potential antiresorption bone drugs
Chiminazzo, Andrea,Sperni, Laura,Damuzzo, Martina,Strukul, Giorgio,Scarso, Alessandro
, p. 2712 - 2718 (2015/03/31)
A wide range of gem-bisphosphonate tetraethyl esters as precursors for bisphosphonic acids, which are potent inhibitors of bone resorption, bearing alkyl, aryl, and indole substituents in the β position were prepared through the CuII-catalyzed 1,4-conjugate addition of boronic acids and indoles to vinylidenebisphosphonate tetraethyl ester.
Anti-inflammatory/antiarthritic ketonic bisphosphonic acid esters
Schlachter, Stephen T.,Galinet, Louise A.,Shields, Sharon K.,Aspar, Danielle G.,Dunn, Colin J.,Staite, Nigel D.,Nugent, Richard A.
, p. 1093 - 1096 (2007/10/03)
Bisphosphonate ester 2 is an inhibitor of inflammation, but is devoid of antiarthritic effects. SAR studies on a series of related bisphosphonate esters resulted in compounds 6e, 6i, 6j, and 6m, which exhibited excellent inhibition of an arthritis model, in addition to potent anti-inflammatory effects.
gem-Diphosphonate and gem-phosphonate-phosphate compounds with specific high density lipoprotein inducing activity
Nguyen,Niesor,Bentzen
, p. 1426 - 1433 (2007/10/02)
New diphosphonate compounds and related derivatives were synthesized and investigated for their activity in specifically inducing plasma high density lipoproteins (HDL) and high density lipoprotein cholesterol (HDL-C) in normal rats. The screening of nume
Anti-atherosclerotic pharmaceutical compositions containing diphosphonate compounds
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, (2008/06/13)
The present invention relates to a pharmaceutical composition for increasing the relative quantity of circulating high density lipoproteins favorable augmentating the alpha/beta lipoprotein cholesterol ratios and clearing cholesterol and lipids from certain tissues and inducing hypotensive activity comprising administering to a human an effective amount of a compound of the formula: STR1 where X is H, OH, or STR2 R and R' identical or different are H, CH3 or C2 H5 ; m is zero or 1; and A is selected from the group comprising (CH3)3 C--, Y--C6 H4 --, Y--C6 H4 --O--C(CH3)2 --, Y--C6 H4 --C(CH3)2 --, Y--C6 H4 --C(O)--C6 H4 --, Y--C6 H4 --(CH2)n -- and Y--C6 H4 --O--(CH2)n --, where n is an integer from 1 to 6 and Y is H, CH3, OCH3, a halogen, and a pharmaceutically acceptable excipient.
