Abstract: Pharmaceutical compositions for the treatment of hypertension comprising an effective anti-hypertensive amount of at least one compound in association with a pharmaceutically acceptable, substantially non-toxic carrier or excipient, the compound having one of the formulae (I), (II), (III) or (IV), and methods for the treatment of hypertension or effecting anti-hypertensive action which comprises administering to a patient requiring anti-hypertensive therapy or effect at least one of the above-described compounds.

Abstract: A method and composition for treating irritable bowel syndrome in a subject in need of such treatment, utilizing an amount of a polyamine having the formula: 1) R—NH—(CH2)a—NH—(CH2)bH—(CH2)c—NH2, 2) CF3—C6H5—(CH2)a—NH—(CH2)b—NH—(CH2)c—NH—(CH2)d—NH—(CH2)e—C6H5—CF3, 3) R—NH—(CH2)a—NH—C6H6—NH—(CH2)b—NH—R and 4) PIP—(CH2)aNH—(CH2)b—NH—(CH2)c—PIP, wherein: R is alkyl, aryl, aralkyl, alkaryl, or cyclo-alkyl having up to about 10 carbon atoms, and any of the alkyl chains may optionally be interrupted by at least one etheric oxygen atom, PIP is piperidine and a, b, c, d, and e may be the same or different and are integers from 1-10 effective to treat irritable bowel syndrome.

Abstract: A composition in unit dosage form for the inhibition, prevention or treatment of inflammatory bowel disease comprising an effective amount of a compound having the formula: and a pharmaceutically acceptable carrier therefor.

Abstract: A method and composition for treating irritable bowel syndrome in a subject in need of such treatment, utilizing an amount of a polyamine having the formula: RNH—(CH2)aNH(CH2)bNH(CH2)cNH2,  1) CF3—C6H5—(CH2)a—NH—(CH2)b—NH—(CH2)c—NH—(CH2)d—NH—(CH2)e—C6H5—CF3,  2) R—NH—(CH2)a—NH—C6H6—NH—(CH2)b—NH—R and  3) PIP—(CH2)aNH—(CH2)b—NH—(CH2)c—PIP,  4) wherein: R is alkyl, aryl, aralkyl, alkaryl, or cyclo-alkyl having up to about 10 carbon atoms, and any of the alkyl chains may optionally be interrupted by at least one etheric oxygen atom, PIP is piperidine and a, b, c, d, and e may be the same or different and are integers from 1-10 effective to treat irritable bowel syndrome.

Abstract: The use of a novel mono-cationic salt of N,N′-bis(2-hydroxybenzyl) ethylenediamine-N,N′-diacetic acid (HBED) in iron chelating therapy is disclosed. In particular, the invention relates to the subcutaneous use of a mono cationic salt of HBED for treating a human with a disease treatable by an iron chelator such as iron overload, especially transfusional iron overload.

Abstract: The invention relates to novel peptides synthesized according a method utilizing the hypusine reagent: wherein: Q1 Q2 and Q3 may be the same or different and are amino protective groups, provided that Q3 is orthogonal to Q1 and Q2; and Z is a hydroxy protective group, as well as improved methods of peptide synthesis wherein the above-described hypusine reagent is employed to prepare novel hypusine-containing peptides.

Abstract: The invention relates to novel peptides synthesized according a method utilizing the hypusine reagent: wherein: Q1 Q2 and Q3 may be the same or different and are amino protective groups, provided that Q3 is orthogonal to Q1 and Q2; and Z is a hydroxy protective group, as well as improved methods of peptide synthesis wherein the above-described hypusine reagent is employed to prepare novel hypusine-containing peptides.

Abstract: Polyamines having the formula: wherein R1 and R2 are alkyl, aralkyl or aryl having up to 10 carbon atoms; and a and b may be the same or different and are integers from 1 to 8; or a salt thereof with a pharmaceutically acceptable acid. Anti-neoplastic, anti-diarrheal, anti-peristaltic, gastro-intestinal anti-spasmodic, anti-viral, anti-retroviral, anti-psoriasis and insecticidal compositions comprising biologically effective amounts of the above-described amines and biologically acceptable carriers therefor are also disclosed, as well as methods of treatment, administration or application of biologically effective amounts of the polyamines of the invention. Also disclosed are methods for preparing the polyamines of the invention.

Abstract: A method and composition for treating irritable bowel syndrome in a subject in need of such treatment, utilizing an amount of a polyamine having the formula: R—NH—(CH2)a—NH—(CH2)bH—(CH2)c—NH2,  1) CF3—C6H5—(CH2)a—NH—(CH2)b—NH—(CH2)c—NH—(CH2)dNH—(CH2)e—C6H5—CF3,  2) R—NH—(CH2)a—NH—C6H6—NH—(CH2)b—NH—R  3) and PIP—(CH2)a—NH—(CH2)b—NH—(CH2)c—PIP,  4) wherein: R is alkyl, aryl, aralkyl, alkaryl, or cyclo-alkyl having up to about 10 carbon atoms, and any of the alkyl chains may optionally be interrupted by at least one etheric oxygen atom, PIP is piperidine and a, b, c, d, and e may be the same or different and are integers from 1-10 effective to treat irritable bowel syndrome.

Abstract: Anti-diarrheal, anti-secretory, nitric oxide agonist, nitric oxide synthase activating or gastrointestinal anti-spasmodic compounds of the formula:  R1—N1H—(CH2)3—N2H—(C2)3—N3H—(CH2)4—N4H—(CH2)3—N5H—(CH2)3—N6H—R6  (II); or wherein: R1 and R6 may be the same or different and are H, alkyl or aralkyl having from 1 to 12 carbon atoms; R2-R5 may be the same or different and are H, R1 or R6; R7 is H, alkyl, aryl or aralkyl having from 1 to 12 carbon atoms; m is an integer from 3 to 6, inclusive; and n is an integer from 3 to 6, inclusive; or (IV) a salt thereof with a pharmaceutically acceptable acid; and a pharmaceutically acceptable carrier therefor. Methods of treatment utilizing the composition are also disclosed.

Abstract: Polyamines having the formula: 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

Abstract: Pharmaceutical compositions for the treatment of cardiac arrhythmia comprising an effective anti-arrhythmic amount of at least one compound in association with a pharmaceutically acceptable, substantially non-toxic carrier or excipient, the compound having one of the formulae (I) or (II) or a salt thereof with a pharmaceutically acceptable acid, and methods for the treatment of cardiac arrhythmia or effecting anti-arrhythmia action which comprise administering to a patient requiring anti-arrhythmic therapy or effect at least one of the above-described compounds.

Abstract: A method and pharmaceutical composition for inhibiting or preventing the intracellular biosynthesis of EIf5A by the administration to a human or non-human mammal in need thereof an amount of a polyamine analogue or salt thereof sufficient to deplete the supply of intracellular spermidine required for EIf5A biosynthesis.

Abstract: Polyamines having the formula: wherein R1 and R2 are alkyl, aralkyl or aryl having up to 10 carbon atoms; and a and b may be the same or different and are integers from 1 to 8; or a salt thereof with a pharmaceutically acceptable acid. Anti-neoplastic, anti-diarrheal, anti-peristaltic, gastro-instestinal anti-spasmodic, anti-viral, anti-retroviral, anti-psoriasis and insecticidal compositions comprising biologically effective amounts of the above-described amines and biologically acceptable carriers therefor are also disclosed, as well as methods of treatment, administration or application of biologically effective amounts of the polyamines of the invention. Also disclosed are methods for preparing the polyamines of the invention.

Abstract: The invention relates to a method and reagent for the synthesis of peptides containing deoxyhypusine, the reagent having the formula: wherein: Q1 and Q2 may be the same or different and are amino protective groups, and Q3 is an amino protective group which is orthogonal to Q1 and Q2. The invention also relates to peptides of formula S-deoxyHpu-T  (2) that may be synthesized using the reagent of the invention, wherein deoxyHpu is the deoxyhypusine residue, S and T are each independently peptide residues from zero to 12 amino acids in length.

Abstract: A derivative of hypusine useful as a reagent for synthesizing peptides containing hypusine, as well as an improved method for synthesizing the same, the derivative having the formula: wherein: Q1 and Q2 may be the same or different and are amino protective groups; Q3 is an amino protective group which is orthogonal to Q1 and Q2; and Z is a hydroxy protective group.

Abstract: The use of a novel mono-cationic salt of N,N′-bis(2-hydroxybenzyl)ethylenediamine-N,N′-diacetic acid (HBED) in iron chelating therapy is disclosed. In particular, the invention relates to the subcutaneous use of a mono cationic salt of HBED for treating a human with a disease treatable by an iron chelator such as iron overload, especially transfusional iron overload.

Abstract: Polyamines having the formula: or a salt thereof with a pharmaceutically acceptable acid wherein: R1-R5 may be the same or different and are alkyl, aryl, aryl alkyl, cycloalkyl or hydrogen; at least one of R1 and R2 and at least one of R4 and R5 are not hydrogen, and any of the alkyl chains may optionally be interrupted by at least one etheric oxygen atom, excluding N1,N3-diethylspermidine and N1,N3-dipropylspermidine; and A and B are bridging groups 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; and (ii) upon uptake by the target cell, competitively binds 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.

Abstract: Polyamines having the formula: 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

Abstract: The present invention relates to anti-neoplastic and anti-psoriasis pharmaceutical compositions and methods of treatment and to insecticidal compositions and methods of controlling the growth of insects.