Diphosphonates

Details Diphosphonates Diphosphonates

1980-01-22

1982-01-05

Sutto, Anton H.

Chemistry of carbon compounds

Dipeptides, e.g., aspartame, anserine, carnosine, etc.

260932, 2605024P, 424204, C07F 911, C07F 940, A61K 3166

Patent

active

043093647

ABSTRACT:
This invention relates to new diphosphonate compounds of formula (I) ##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 --CO--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. These compounds 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.

REFERENCES:
patent: 2848475 (1958-08-01), Schmidt
patent: 3299123 (1967-01-01), Fitch et al.
patent: 3463835 (1969-08-01), Budnick
patent: 3471406 (1969-10-01), Budnick
patent: 4067971 (1978-01-01), Francis et al.
patent: 4113861 (1978-09-01), Fleisch et al.
patent: 4137309 (1979-01-01), Van Duzee
Puddvik et al., "Index Chemicus," vol. 28, (1968), #89485.
Nicholson et al., "J. Org. Chem.", vol. 36, No. 24, (1971), pp. 3843-3845.

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