Abstract: A method of chemically resecting the exocrine portion of the pancreas of a patient in need thereof comprising administering to the patient an amount of a hydroxy polyamine or a salt thereof with a pharmaceutically acceptable acid sufficient to resect the exocrine portion of the pancreas thereof, but insufficient to substantially alter the endocrine portion thereof. The hydroxy polyamine has a structure according to the formula: ##STR1## wherein: R.sub.1 and R.sub.2 may be the same or different and are alkyl having 1 to 6 carbon atoms or aryl or aralkyl having up to 12 carbon atoms;a, b, d and e may be the same or different and are integers from 1 to 4; andc is an integer from 2 to 6.A pharmaceutical composition in unit dosage form comprising the hydroxy polyamine or a salt thereof with a pharmaceutically acceptable acid for use in the method of the invention is also disclosed.

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: ##STR1## and a pharmaceutically acceptable carrier therefor.

Abstract: Phenyl- and pyridyl-substituted thiazoline acid derivatives useful in diagnosing and treating pathological conditions associated with an excess of trivalent metals in humans and animals.

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-arrhythmic action which comprise administering to a patient requiring anti-arrhythmic therapy or effect at least one of the above-described compounds.

Abstract: A derivative of hypusine useful as a reagent for synthesizing peptides containing hypusine, as well as a method for synthesizing the same, the derivative having the formula: ##STR1## wherein: Q.sub.1 and Q.sub.2 may be the same or different and are amino protective groups;Q.sub.3 is an amino protective group which is orthogonal to Q.sub.1 and Q.sub.2 ; andZ is a hydroxy protective group.

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.

Abstract: Polyamines having the formula: ##STR1## wherein R.sub.1 and R.sub.2 are alkyl, aralkyl or aryl having up to 10 carbon atoms; anda and b may be the same or different and are integers from 1 to 8; ora 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: 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: R.sub.1 and R.sub.6 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;N.sup.1, N.sup.2, N.sup.3 and N.sup.4 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.

Abstract: Methods for treating inflammatory conditions wherein the active agent is a polyamine having the formula set forth below: ##STR1## or a salt thereof with a pharmaceutically acceptable acid wherein: R.sub.1, R.sub.2, R.sub.3 and R.sub.4 may be the same or different and represent H, straight- or branched-chain alkyl, aryl, aryl alkyl or cycloalkyl of 1-12 carbon atoms;a, b, c and d may be the same or different and are integers from 0 to 8, except that when a or c is zero, b or d is greater than or equal to 3 and when a or c is one, b or d is greater than or equal to 2; andX, Y and Z may be the same or different; X and Z are integers from 0 to 10; and Y is an integer from 1 to 10, excluding the polyamine of the formula wherein a=b=c=d=2, X=Z=2 and Y=4.

Abstract: Thiazoline acids and derivatives useful as chelators of trivalent metals in therapeutic applications have been prepared.

Abstract: A method of synthesizing rhizoferrin and analogues thereof comprising acylating a protected polyamine with a citric acid diester; hydrolyzing the resulting amide to produce an N-protected rhizoferrin or analog thereof; and de-protecting the intermediate to produce rhizoferrin or the analog thereof.

Abstract: Anti-diarrheal, anti-secretory, nitric oxide agonist, nitric oxide synthase activating or gastrointestinal anti-spasmodic compounds of the formula: ##STR1## wherein: R.sub.1 and R.sub.6 may be the same or different and are H, alkyl or aralkyl having from 1 to 12 carbon atoms;R.sub.2 -R.sub.5 may be the same or different and are H, R.sub.1 or R.sub.6 ;R.sub.7 is H, alkyl, aryl or aralkyl having from 1 to 12 carbon atoms;m is an integer from 3 to 6, inclusive; andn 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: ##STR1## wherein R.sub.1 and R.sub.2 are alkyl, aralkyl or aryl having up to 10 carbon atoms; anda 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, gastrointestinal 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: Polyamines having the formula: ##STR1## wherein R.sup.1 and R.sub.2 are alkyl, aralkyl or aryl having up to 10 carbon atoms; anda and b may be the same or different and are integers from 1 to 8; ora salt thereof with a pharmaceutically acceptable acid. Anti-neoplastic, anti-diarrheal, anti-peristaltic, gastrointestinal 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: 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), or (II), 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 new and versatile route to N'-[5-[[4-[[5-(acetylhydroxyamino)pentyl]amino]-1,4-dioxobutyl]hydroxyamin o]pentyl]-N-(5-aminopentyl)-N-hydroxybutanediamide, desferrioxamine B (DFO) is described. N-Benzyloxy-1,5-diaminopentane is selectively protected at the primary amino site. The product is reacted at the benzyloxyamine with an anhydride to produce a carboxylic acid which is, in turn, acylated regio-specifically with a diamine at the primary amine to give a benzyloxyamine. The previous two steps are repeated to afford a DFO reagent. Acetylation of the DFO reagent, followed by hydrogenolysis and tert-butoxycarbonyl group removal, furnishes DFO.

Abstract: Anti-diarrheal, anti-secretory, nitric oxide agonist, nitric oxide synthase activating or gastrointestinal anti-spasmodic compounds of the formula: ##STR1## wherein: R.sub.1 and R.sub.6 may be the same or different and are H, alkyl or aralkyl having from 1 to 12 carbon atoms;R.sub.2 -R.sub.5 may be the same or different and are H, R.sub.1 or R.sub.6 ;R.sub.7 is H, alkyl, aryl or aralkyl having from 1 to 12 carbon atoms;m is an integer from 3 to 6, inclusive; andn 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: Anti-diarrheal, anti-secretory, nitric oxide agonist, nitric oxide synthase activating or gastrointestinal anti-spasmodic compounds of the formula: ##STR1## wherein: R.sub.1 and R.sub.6 may be the same or different and are H, alkyl or aralkyl having from 1 to 12 carbon atoms;R.sub.2 -R.sub.5 may be the same or different and are H, R.sub.1 or R.sub.6 ;R.sub.7 is H, alkyl, aryl or aralkyl having from 1 to 12 carbon atoms;m is an integer from 3 to 6, inclusive; andn 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: Synthesis of desferrioxamine B and analogs and homologs thereof beginning with O-protected, N-protected hydroxylamine, which is N-alkylated to produce a protected N-4-cyanoalkylhydroxylamine which is acylated with a suitable anhydride. The resulting half-acid amide is subjected to a series of high yield condensations and reductions which vide desferrioxamine B in high overall yield. Alternatively, polyether analogs of desferrioxamine B can be prepared by reacting an activated polyether with the O-protected, N-protected hydroxylamine and subjecting the resulting product to a series of similar steps.

Abstract: The invention relates to novel analogs of desferrioxamine, homologs thereof and methods for their synthesis.