Abstract: Provided herein are combinations comprising difluoromethylornithine (DFMO), or an ionic form thereof, and a compound of the following structural formula: or a protonated form thereof, wherein values for the variables (e.g., a, b, c, d, e, n, R1, R2, X) are described herein. The combinations can provide combination drug therapy in a single pharmaceutical dosage form, and be used, for example, for the treatment of cancer.

Abstract: Provided herein are methods of treating cancer, comprising administering AMXT 1501, or a pharmaceutically acceptable salt thereof, orally, and difluoromethylornithine (DFMO), or a pharmaceutically acceptable salt thereof, intravenously to a subject in need thereof.

Abstract: Disclosed herein are pharmaceutical salts of a cationic protonated polyamine pharmaceutical agent and an anionic organic carboxylate which is hydrophobic when in protonated form, particularly suited for oral administration, where these salts have good bioavailability in solid dosage forms and may be used in the treatment of cancer and other medical conditions for which the pharmaceutical agent is intended.

Abstract: Disclosed herein are pharmaceutical salts of a cationic protonated polyamine pharmaceutical agent and an anionic organic carboxylate which is hydrophobic when in protonated form, particularly suited for oral administration, where these salts have good bioavailability in solid dosage forms and may be used in the treatment of cancer and other medical conditions for which the pharmaceutical agent is intended.

Abstract: Provided herein are combinations comprising difluoromethylornithine (DFMO), or an ionic form thereof, and a compound of the following structural formula: or a protonated form thereof, wherein values for the variables (e.g., a, b, c, d, e, n, R1, R2, X) are described herein. The combinations can provide combination drug therapy in a single pharmaceutical dosage form, and be used, for example, for the treatment of cancer.

Abstract: Disclosed herein are pharmaceutical salts of a cationic protonated polyamine pharmaceutical agent and an anionic organic carboxylate which is hydrophobic when in protonated form, particularly suited for oral administration, where these salts have good bioavailability in solid dosage forms and may be used in the treatment of cancer and other medical conditions for which the pharmaceutical agent is intended.

Abstract: Disclosed herein are pharmaceutical salts of a cationic protonated polyamine pharmaceutical agent and an anionic organic carboxylate which is hydrophobic when in protonated form, particularly suited for oral administration, where these salts have good bioavailability in solid dosage forms and may be used in the treatment of cancer and other medical conditions for which the pharmaceutical agent is intended.

Abstract: Disclosed herein are pharmaceutical salts of a cationic protonated polyamine pharmaceutical agent and an anionic organic carboxylate which is hydrophobic when in protonated form, particularly suited for oral administration, where these salts have good bioavailability in solid dosage forms and may be used in the treatment of cancer and other medical conditions for which the pharmaceutical agent is intended.

Abstract: This disclosure demonstrates a novel therapy immunological approach using polyamine-based therapy (PBT) for relieving tumor-induced suppression of the patient's immune system. The demonstration of the pharmacological release from the naturally occurring polyamine-mediated immune suppression offers profound impact on the immunotherapy of cancer together with a variety of diseases caused by the disease-causing vector's ability to evade an immune reaction. This therapeutic approach is equally applicable to disease states whereby immune system suppression by polyamines has been demonstrated including; bacterial infections, parasitic infections including malaria and typanosomiasis, viral infections, peptic ulcers and gastric cancer due to H. Pylori infection together with prevention of pregnancy. With a small molecule drug, used in combination with DFMO, the pharmacological manipulation of polyamine levels for therapeutic benefit in various disease states is possible.

Abstract: This disclosure demonstrates a novel therapy immunological approach using polyamine-based therapy (PBT) for relieving tumor-induced suppression of the patient's immune system. The demonstration of the pharmacological release from the naturally occurring polyamine-mediated immune suppression offers profound impact on the immunotherapy of cancer together with a variety of diseases caused by the disease-causing vector's ability to evade an immune reaction. This therapeutic approach is equally applicable to disease states whereby immune system suppression by polyamines has been demonstrated including; bacterial infections, parasitic infections including malaria and typanosomiasis, viral infections, peptic ulcers and gastric cancer due to H. Pylori infection together with prevention of pregnancy. With a small molecule drug, used in combination with DFMO, the pharmacological manipulation of polyamine levels for therapeutic benefit in various disease states is possible.

Abstract: Small molecule polycationic agents are used to modulate or interrupt biological processes by binding to oligosaccharide-based biomolecules. Compounds that inhibit nitric oxide, TNF? or other immunomodulators are provided and are useful for treating immunological disease and disease of an infectious disorder.

Abstract: Proliferative cutaneous disease states or conditions are treated by administering a polyamine transport inhibitor R-X-L-polyamine wherein R is a straight or branched C10-50 saturated or unsaturated aliphatic, carboxyalkyl, carbalkoxyalkyl, or alkoxy; a C1-8 alicyclic; a single or multiring aryl substituted or unsubstituted aliphatic; and aliphatic-substituted or unsubstituted single or multiring aromatic; a single or multiring heterocyclic; a single or multiring heterocyclic aliphatic; an aryl sulfonyl; X is —CO—, —SO2—, or —CH2—; and L is a covalent bond or a naturally occurring amino acid, lysine, ornithine, 2,4-diaminobutyric acid, or pharmaceutically acceptable salts thereof or prodrug thereof, and a polyamine biosynthesis inhibitor.

Abstract: Certain lipophilic polycationic sulfonamides are provided and are useful for treating various diseases or conditions and particularly sepsis.

Abstract: The synthesis and use of a novel class of tumor necrosis factor (TNF?) inhibitors and immunomodulators are provided. Examples are those having the structures: wherein a, b and c are integers from 0 to 12, X equals NH or CHNH2, R1 and R2 each is a hydrogen or a C1 to C20 aliphatic; aliphatic amine; an alicyclic; aromatic; heterocycle; and halogenated forms thereof; and wherein, a, b and c are integers from 0 to 12; R1, R2, R3, and R4 each is a hydrogen or a C1 to C20; aliphatic amine; an alicyclic; aromatic; a heterocycle; and halogenated forms thereof.

Abstract: Certain lipophilic polycationic sulfonamides are provided and are useful for treating various diseases or conditions and particularly sepsis.

Abstract: Tetrahydro-?-carboline compounds represented by the following formulae: wherein x, y and z are each independently an integer of 0 to 4 and R is selected from the group consisting of H, alkyl, aryl and heterocyclic moiety wherein the alkyl, aryl and heterocyclic moiety are optionally substituted with a member selected from the group consisting of halogen, alkoxy and trifluoromethyl; pharmaceutically acceptable salts thereof and prodrugs thereof are provided. The compounds are useful for treating neurological diseases.

Abstract: Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. Novel chemical synthetic methods to obtain polyamine analogues are disclosed, including the production of a combinational polyamine library. These approaches yield analogues with desirable activities both for diagnostic and research assays and therapy. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that interact with the polyamine system.

Abstract: Small molecule polycationic agents are used to modulate or interrupt biological processes by binding to oligosaccharide-based biomolecules. Compounds that inhibit nitric oxide, TNF? or other immunomodulators are provided and are useful for treating immunological disease and disease of an infectious disorder.

Abstract: Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. Novel chemical synthetic methods to obtain polyamine analogues are disclosed, including the production of a combinatiorial polyamine library. These approaches yield analogues with desirable activities both for diagnostic and research assays and therapy. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that interact with the polyamine system.

Abstract: The disclosed invention provides new polyamine analogs and derivatives containing a hydrophobic region and a polyamine region as well as methods and compositions for their use.