Symphar S.a.

Lan Nguyen Mong

Eric Joseph Niesor

Craig Leigh Bentzen

Hieu Trung Phan

Yves Guyon-Gellin

Kyriacos Kalathakis

Jean-Robert Rossier

2-Substituted-1,3-propylidenediphosphonates of formula (I), where A, R.sup.1 and R.sup.2 are defined in claim 1, are therapeutically active compounds, namely for the treatment of cardiovascular diseases. They can be prepared by reacting phosphonating agents with 1,3- dibromopropanes or ditosylates of 1,3-propanediols substituted in position 2. ##STR1## .

Certain 2-substituted 1,3-propylidenediphosphonate derivatives,

A method of increasing the quantity of circulating high density lipoproteins and clearing cholesterol from certain tissues, comprising administering to a human an effective amount of a compound of the formula ##STR1## where X is H, OH, ##STR2## or NH.sub.2 ; R and R' identical or different are H, CH.sub.3 or C.sub.2 H.sub.5 ; m is zero or 1; and A is selected from the group comprising (CH.sub.3).sub.3 C--, Y--C.sub.6 H.sub.4 --, Y--C.sub.6 H.sub.4 --O--C(CH.sub.3).sub.2 --, Y--C.sub.6 H.sub.4 --C(CH.sub.3).sub.2 --, Y--C.sub.6 H.sub.4 --C(O)--C.sub.6 H.sub.4 --, Y--C.sub.6 H.sub.4 --(CH.sub.2).sub.n -- and Y--C.sub.6 H.sub.4 --O--(CH.sub.2).sub.n --, where n is an integer from 1 to 6 and Y is H, CH.sub.3, OCH.sub.3 or Cl.

Therapeutic process with diphosphonate compounds

This invention relates to new monophosphonate compounds of formula X--C.sub.6 H.sub.4 --(O).sub.m --(CH.sub.2).sub.n --R where R is --PO.sub.3 Me.sub.2, --PO.sub.3 Et.sub.2, --PO.sub.3 H.sub.2 or --PO.sub.3 Na.sub.2, X is a halogen, preferably chlorine, in position o, m or p, preferably in position p; m is 0 or 1; and n is 0, 1, 2, 3, 4, 5 or 6, which possess remarkable activity as hypoglycemic and/or antiatherogenic agents, and are usable in pharmaceutical compositions to alter lipoprotein profiles in favor of high density lipoproteins and to clear cholesterol from various tissues.

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Nyon, Switzerland

Lan Nguyen Mong