Phosphonates as anti-inflammation agents

Details Phosphonates as anti-inflammation agents Phosphonates as anti-inflammation agents

1992-02-11

1993-06-15

Lee, Mary C.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

514114, 514129, 558169, 558186, A61K 31685, A61K 3166

Patent

active

052198456

ABSTRACT:
The invention pertains to the synthesis and use as therapeutic agents of a group of substances with a glycerol backbone or aliphatic chain structure linked to a phosphorus atom and a polar head group. Depending on the polar head group, the substance has anti-cancer, anti-inflammatory, anti-allergy or anti-cardiovascular disease properties. Compounds of the formula: ##STR1## wherein n is 0 to 14 and R.sub.1 is an alkyl group of C.sub.12 -C.sub.20, R.sub.2 is a methyl group, and wherein R.sub.3 is an inositol analog head group, a (CH.sub.2).sub.m N.sup.+ (CH.sub.3).sub.3 group with m=2 to 10, a serine head group, or an ethanolamine head group, or of the formula ##STR2## wherein R.sub.1 and R.sub.2 are as described above, n=0 or 1, and R.sub.3 is (CH.sub.2).sub.m N.sup.+ (CH.sub.3).sub.3 (m=2-10) are claimed. This invention also pertains to the synthesis and use as therapeutic agents of a group of substances that have no glycerol backbone but have an aliphatic chain structure linked directly to a phosphorus atom of the general formula R--P(O)(O.sup.-)OR' wherein R is a long-chain alkyl group such as hexadecyl or octadecyl and R' is a head group such as choline, glycerol, inositol, ethanolamine, or serine.

REFERENCES:
patent: 4408052 (1983-10-01), Hozumi et al.
patent: 4515722 (1985-05-01), Yang et al.
Chem. Abstr. 1985, 103(21), 178451f; Japan Kokai Tokkyo Koho 60-069088.

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