Bisphosphonates, pharmaceutical compositions, and process for th

Details Bisphosphonates, pharmaceutical compositions, and process for th Bisphosphonates, pharmaceutical compositions, and process for th

1991-09-23

1993-03-23

Lee, Mary C.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Phosphorus containing other than solely as part of an...

558158, 558161, 562 20, A61K 3166, C07F 940, C07F 938

Patent

active

051964090

ABSTRACT:
Novel bisphosphonates comprise compounds of the formula (I) ##STR1## wherein m and l are independently 1 or 2; R.sub.1 represents hydrogen, a lower alkyl group, or an alkali metal cation; R.sub.2 represents hydrogen, a lower alkyl group or an alkali metal cation; Y represents .dbd.0 or .dbd.N--OH, or --OH; and X represents --(CH.sub.2).sub.n --, a branched alkylene group, or a branched or straight alkenylene or alkynylene chain optionally substituted by one or more oxygen or nitrogen atoms, wherein n is an integer from 3 to 24; with the provision that when l.dbd.m.dbd.1, Y is .dbd.0, and R.sub.1 and R.sub.2 denote a lower alkyl group, n represents an integer from 9 to 20; and with the provision that when l.dbd.m.dbd.2, Y is --OH and R.sub.1 and R.sub.2 are methyl groups, n represents an integer from 9-24; and with the further provision that when l.dbd.m.dbd.2, Y is --OH and R.sub.1 and R.sub.2 are hydrogen, n represents 3, 5 or an integer from 7 to 24; or X is

REFERENCES:
patent: 3012054 (1961-12-01), Moss et al.
Rafik Karaman et al., Acylphosphonic Acids and Methyl Hydrogen Acylphosphonates: Physical and Chemical Properties and Theoretical Calculations, J. Chem. Soc. 1989.
Kanaan et al., Phosphorous and Sulfur, 1988, vol. 37, pp. 217-229.
Hilderbrand, CRC, "The Role of Phosphonates in Living Systems", pp. 55-96 1980.
Hilderbrand, CRC, "The Role of Phosphonates in Living Systems", pp. 161-188 1980.

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