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US 5,962,533 AGranted
Hydroxy polyamines
AssigneeUniversity of Florida Research Foundation, Inc.
InventorRaymond J. Bergeron, Jr.
Life of this patent
Estimating the term…
Abstract
Disclosed are polyamines having the formula: ##STR1## or salts or stereoisomers thereof wherein R.sub.1 -R.sub.4 and ALK.sub.1 -ALK.sub.3 are as defined in the specification. Pharmaceutical compositions and therapeutic methods of treatment utilizing the compounds are also disclosed.
Claims7
A polyamine having the formula:
- ##STR38## or its possible stereoisomers or a salt thereof with a pharmaceutically acceptable acid wherein:
- R.sub.1 and R.sub.4 may be the same or different and are alkyl, aryl, aryl alkyl or cycloalkyl, optionally having an alkyl chain interrupted by at least one etheric oxygen atom;
- R.sub.2 and R.sub.3 may be the same or different and are R.sub.1, R.sub.4 or H;
- N.sup.1, N.sup.2, N.sup.3 and N.sup.4 are nitrogen atoms capable of protonation at physiological pH's;
- ALK.sub.1, ALK.sub.2 AND ALK.sub.3 may be the same or different and are straight or branched chain alkylene bridging groups having 1 to 4 carbon atoms which effectively maintain the distance between the nitrogen atoms such that the polyamine:
- (i) is capable of uptake by a target cell upon administration of the polyamine to a human or non-human animal or is capable of binding to at least one polyamine site of a receptor located within or on the surface of a cell upon administration of the polyamine to a human or non-human animal;
- and
- (ii) upon uptake by the target cell, competitively binds via an electrostatic interaction between the positively charged nitrogen atoms to biological counter-anions;
- the polyamine, upon binding to the biological counter-anion in the cell, functions in a manner biologically different than the intracellular polyamines;
- and
- further wherein at least one of said bridging groups ALK.sub.1, ALK.sub.2 and ALK.sub.3 contains at least one --CH(OH)-- group which is not alpha- to either of the nitrogen atoms.
8 more elements
Dependencies are inferred from the claim text.