초록 ▼

Polyamines having the formula: [EQU1]or 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 n

Polyamines having the formula: [EQU1]or 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.

대표청구항 ▼

1. A polyamine having the formula: [EQU15]or 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 chains interrupted by at least one etheric oxygen atom, or hydrogen N1, N2, N3 and N4

1. A polyamine having the formula: [EQU15]or 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 chains 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 said nitrogen atoms such that said polyamine: (i) is capable of uptake by a target cell upon administration of said polyamine to a human or non-human animal; and (ii) upon uptake by said target cell, competitively binds via an electrostatic interaction between the positively charged nitrogen atoms to substantially the same biological counter-anions as the intra-cellular natural polyamines in the target cell; said polyamine, upon binding to said biological counter-anion in the cell, functions in a manner biologically different than said intracellular polyamines, said polyamine not occurring in nature.