- Analogs of biologically active, naturally occurring polyamines, pharmaceutical compositions and methods of treatment
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Polyamines having the formula: 1or a salt thereof with a pharmaceutically acceptable acid wherein: R1-R6 may be the same or different and are alkyl, aryl, aryl alkyl, cycloalkyl, optionally having an alkyl chain interrupted by at least one etheric oxygen atom, or hydrogen; N1, N2, N3 and N4 are nitrogen atoms capable of protonation at physiological pH's; a and b may be the same or different and are integers from 1 to 4; A, B and C may be the same or different and are bridging groups which effectively maintain the distance between the nitrogen atoms such that the polyamines: (i) are capable of uptake by a target cell upon administration thereof to a human or non-human animal; and (ii) upon uptake by the target cell, competitively bind via an electrostatic interaction between the positively charged nitrogen atoms to substantially the same biological counter-anions as the intracellular natural polyamines in the target cell; the polyamines, upon binding to the biological counter-anion in the cell, function in a manner biologically different than the intracellular polyamines, the polyamines not occurring in nature; as well as pharmaceutical compositions embodying the polyamines and methods of treating patients requiring anti-neoplastic therapy.
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- Analogs of biologically active, naturally occurring polyamines, pharmaceutical compositions and methods of treatment
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Polyamines having the formula: or a salt thereof with a pharmaceutically acceptable acid wherein: R1-R6may be the same or different and are alkyl, aryl, aryl alkyl, cycloalkyl, optionally having an alkyl chain interrupted by at least
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Page column 12-13
(2010/01/30)
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- Methods and compositions for the treatment of neurodegeneration
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Methods and pharmaceutical compositions in unit dosage form for treating neurodegeneration in a human or non-human animal afflicted therewith wherein the active agent is a therapeutically effective amount of a polyamine having the formula: STR1 or a salt thereof with a pharmaceutically acceptable acid wherein: R1 and R6 may be the same or different and are hydrogen, alkyl, hydrocarbyl aryl, hydrocarbyl aryl alkyl, cycloalkyl, or any of the foregoing wherein the alkyl chain is interrupted by at least one etheric oxygen atom; N1, N2, N3 and N4 are nitrogen atoms capable of protonation at physiological pH's; a and b may be the same or different and are integers from 1 to 4; A, B and C may be the same or different and are bridging groups of variable length.
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- Antiproliferative Properties of Polyamine Analogues: A Structure-Activity Study
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A basis set of polyamine analogues was designed and synthesized.These compounds were used to initiate a systematic investigation of the role of chain length, terminal nitrogen alkyl group size, and symmetry of the methylene backbone in the antineoplastic
- Bergeron, Raymond J.,McManis, James S.,Liu, Charles Z.,Feng, Yang,Weimar, William R.,et al.
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p. 3464 - 3476
(2007/10/02)
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