Enhanced anti-angiogenic activity of permanently charged derivatives of steroid hormones
AssigneePharmos Corporation
InventorsAnat Biegon, Marcus E. Brewster
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Abstract
The present invention discloses the use of permanently charged steroid agonists or antagonists as potent anti-angiogenic compositions comprising as an active ingredient a compound of the general formulae I, II or III: wherein DRUG is any steroid agonist or antagonist, a mixed agonist-antagonist, or a partial agonist and the substituents are as defined in the specification.
Claims19
A method for treating a medical condition which involves angiogenesis in a subject, which comprises administering to a subject in need of such treatment a therapeutically effective amount of a pharmaceutical composition having anti-angiogenic activity which contains as an active ingredient a therapeutically effective quantity of a compound of the formula (I):
- wherein:
- Y is a non-toxic pharmaceutically acceptable anion;
- DRUG is a radical selected from the group consisting of a steroid agonist or antagonist, a mixed agonist-antagonist, and a partial agonist;
- X is a direct bond or a radical selected from the group consisting of —O—;
- —NH—;
- —NR—, wherein R is an alkyl or aryl group with less than ten carbons;
- —PO3—;
- —S—;
- —SO—;
- and —SO2—;
- R1 and R2 are the same or different and may be a radical selected from the group consisting of H, an alkyl of 1-10 carbon atoms, an arylalkyl of 7-16 carbons, and an aryl;
- R3, R4 and R5 are independently a radical selected from the group consisting of a branched or unbranched, cyclic or noncyclic, alkyl of 1-10 carbon atoms;
- an alkyl of up to 10 carbon atoms substituted by a carboxy, hydroxy, alkoxy, halo, or nitro group;
- a branched or unbranched, cyclic or noncyclic arylalkyl of 7-16 carbon atoms;
- and an aryl;
- and
- n is 0-12.
Dependencies are inferred from the claim text.