Abstract: Peptide conjugates in which cytocidal and cytostatic agents, such as polyamine analogs or naphthoquinones, are conjugated to a polypeptide recognized and cleaved by enzymes such as prostate-specific antigen (PSA) and cathepsin B are provided, as well as compositions comprising these conjugates. Methods of using these conjugates in the treatment of prostate diseases are also provided.

Abstract: Novel “bispolyamine” inhibitor compounds of polyamine transport are disclosed. These compounds 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. These compounds display desirable activities both for diagnostic and research assays and therapy.

Abstract: Methods are provided for reducing copper values for, by way of example, treating, preventing or ameliorating tissue damage such as, for example, tissue damage that may be caused by (i) disorders of the heart muscle (for example, cardiomyopathy or myocarditis) such as idiopathic cardiomyopathy, metabolic cardiomyopathy which includes diabetic cardiomyopathy, alcoholic cardiomyopathy, drug-induced cardiomyopathy, ischemic cardiomyopathy, and hypertensive cardiomyopathy, (ii) atheromatous disorders of the major blood vessels (macrovascular disease) such as the aorta, the coronary arteries, the carotid arteries, the cerebrovascular arteries, the renal arteries, the iliac arteries, the femoral arteries, and the popliteal arteries, (iii) toxic, drug-induced, and metabolic (including hypertensive and/or diabetic disorders of small blood vessels (microvascular disease) such as the retinal arterioles, the glomerular arterioles, the vasa nervorum, cardiac arterioles, and associated capillary beds of the eye, the kidney

Abstract: The invention provides novel polyamine compounds and pharmaceutical compositions for administration in conjunction with cancer chemotherapy or radiation therapy. The compounds are administered locally to provide protection against the adverse side-effects of chemotherapy or radiation therapy, such as alopecia, mucositis and dermatitis. Pharmaceutical preparations comprising one or more chemoprotective polyamines formulated for topical or local delivery to epithelial or mucosal cells are disclosed. Methods of administering the pharmaceutical preparations are also disclosed.

Abstract: The present invention provides methods and compositions for modulating polyamine pathway activity as a means for ameliorating neurodegenarative disorders. In particular, for ameliorating the symptoms or onset of amyotrophic lateral sclerosis (ALS) by modulating the gene and protein products involved the polyamine pathway, such as by inhibiting the enzyme, ornithine decarboxylase (ODC), involved in the synthesis of the polyamine, putrescine. Compositions and methods are disclosed for inhibiting the polyamine pathway producing lower polyamine levels resulting in a beneficial effect on ALS. This can be accomplished by using modulating agents such as analogs, or polyamine analogs, and antiproliferative drugs. Screening assays for pharmacological agents that are capable of decreasing polyamine levels and/or reducing cell proliferation are also disclosed.

Abstract: The invention concerns the use of a polyamine derivative or a polyamine for inhibiting the active site of glycosidase enzymes intervening in the transformation of polysaccharides into sugars, in particular into glucose, in a living organism.

Abstract: Compounds of Formula I, and pharmaceutical compositions containing these compounds, activate the insulin receptor kinase, which leads to an increased sensitivity to insulin and an increase in glucose uptake, and are therefore useful for the treatment of animals, especially humans, with hyperglycemia, especially for the treatment of type 2 diabetes. Processes for preparation of the compounds, and their use in assays, are also disclosed.

Abstract: Oligoamine compounds with anti-cancer and anti-proliferative activity are provided, as well as methods for making and using the compounds. The compounds are shown to be active against prostate cancer cell lines and against prostate cancer tumors in mice. The compounds are also useful in treatment of breast cancer and other cancers.

Abstract: The present invention provides methods and compositions for modulating polyamine pathway activity as a means for ameliorating neurodegenarative disorders. In particular, for ameliorating the symptoms or onset of amyotrophic lateral sclerosis (ALS) by modulating the gene and protein products involved the polyamine pathway, such as by inhibiting the enzyme, ornithine decarboxylase (ODC), involved in the synthesis of the polyamine, putrescine. Compositions and methods are disclosed for inhibiting the polyamine pathway producing lower polyamine levels resulting in a beneficial effect on ALS. This can be accomplished by using modulating agents such as analogs, or polyamine analogs, and antiproliferative drugs. In particular, the polyamine analog N(1),N(11)-diethylnorspermine (DENSPM) is disclosed as a useful modulating agent in the treatment of ALS. Screening assays for pharmacological agents that are capable of decreasing polyamine levels and/or reducing cell proliferation are also disclosed.

Abstract: The present invention relates to methods of imprinting fish to be sensitized to an odorant so that modulation of the PVCR in the olfactory apparatus occurs, and then exposing the fish with the same odorant after transfer to seawater or freshwater. The present invention also includes methods of homing or attracting fish, as well as methods for repelling fish by modulating the expression and/or sensitivity of the PVCR in the olfactory apparatus of the fish.

Abstract: Methods and compositions for improving sleep in individuals with sleep disorders or other conditions which interfere with normal sleep via administration of a NO-mimetic are provided.

Abstract: 2,3,2 Tetramine (3,7-diazanonane-1,9-diamine) is propounded for treatment of Parkingson's Disease and dementias characterized by mitochondrial damage in view of this compound's ability to completely neutralize the dopamine-depriving effect of MPTP in laboratory animals up to 12 hours post MPTP injection, and to retain partial protection at suboptimal tissue levels for up to 36 hours.

Abstract: The present invention relates to the use of compounds of the general Formula (I) 1

Abstract: Polyamines having the formula: 1

Abstract: In various aspects, the invention provides methods for treating ocular inflammation using copper chelating compounds, such as compounds other than D-penicillamine. In some embodiments, such compounds may be polyamines, such as triethylenetetramine or tetraethylenepentamine. For example, the present invention provides methods for treating inflammation secondary to ocular laser therapy.

Abstract: A method of treating cancer in a patient deficient in p53 tumor suppression gene is described herein by administering to a patient a therapeutically effective amount if a polyamine such as DENSPM in combination with an anticancer agent. Also described is a method of selecting patients for cancer treatment with a polyamine, for example, DENSPM.

Abstract: The invention relates to the preparation of novel polyamines, such as derivatives of 1,3-bis-[(2′-aminoethyl)-amino]propane (2,3,2-tetramine) and 1,4,8,11-tetraazacyclotetradecane (cyclam), which can be used to treat mitochondrial and degenerative diseases.

Abstract: The present invention provides discrete-length polyethylene glycol and polyethylene glycol containing compounds and methods for their preparation.

Abstract: There is disclosed a class of pharmaceutical compositions useful for the treatment of cancer, particularly solid tumors, and having a mechanism of action as spermine antagonists. The present pharmaceutical compositions are able to inhibit the inhibitory effect of spermine upon macrophage function, and thus prevent spermine-induced immunosuppression.

Abstract: Solvent-free coating materials and treating agents used as water-based wood or material protective agents containing emulsifiable binding agents, quaternary ammonium compounds and optional additional active agents. The wood or material protective agents are non-flammable and enable a uniform distribution of the binding agent and the quaternary ammonium compounds in the substrates. As a result, the quaternary ammonium compounds function as a dissolving mediator for the binding agents which are dispersed in water without opacifying effects and are used as a biocide. The agents can additionally absorb water-insoluble organic biocides without impairing the homogeneity or stability of the formulation of the homogeneity of the distribution in the substrate.

Abstract: Polyamines having the formula: 1

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: Composition in the form of an aqueous solution, useful for disinfecting hard surfaces comprises: a) from 0.0005% to 20% by weight of peracetic acid, b) from 0.001% to 45% by weight of acetic acid, c) from 0.001% to 35% by weight of hydrogen peroxide, d) from 0.0001% to 2% by weight of at least one compound of formula (I) (R1)(R2)(R3)N→O  (I) e) if desired, up to 2.5% by weight of at least one nonionic surfactant, and wherein f) the weight ratio between the compound of formula (I) and the peracetic acid is less than or equal to 1, and in that g) the weight ratio between the nonionic surfactant and the peracetic acid is less than or equal to 0.2.

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.

Abstract: Anti-diarrheal and/or gastrointestinal anti-spasmodic pharmaceutical compositions containing [A] a polyamine of the formula: R1—N1(R2)—(CH2)x—N2H—Q—N3H—(CH2)y—N4(R3)—R4  (I) wherein: R1, R2, R3 and R4 may be the same or different and are H, alkyl, cycloalkyl or aralkyl having from 1 to 12 carbon atoms, or a heterocyclic group having from 3 to 10 atoms wherein the hetero atom is said N1 or N4; Q is a cycloalkyl group having from 3 to 10 carbon atoms; x is an integer from 3 to 6, inclusive; and y is an integer from 3 to 6, inclusive; or (II) a salt thereof with a pharmaceutically acceptable acid; and [B] a pharmaceutically acceptable carrier therefor as well as methods of treatment utilizing the polyamines are disclosed.

Abstract: The present invention discloses highly packed polycationic ammonium, sulfonium and phosphonium lipid compounds useful for making lipid aggregates for delivery of macromolecules and other compounds into cells. They are especially useful for the DNA-dependent transformation of cells. Methods for their preparation and use as intracellular delivery agents are also disclosed.

Abstract: Compounds of Formula I: E—NH—D—NH—B—A—B—NH—D—NH—E  (I) wherein A is C2-C6 alkene, C3-C6 cycloalkyl, cycloalkenyl, or cycloaryl; B is independently a single bond, C1-C6 alkyl alkenyl; D is independently C1-C6 alkyl or alkenyl, or C3-C6 cycloalkyl, cycloalkenyl, or cycloaryl; and E is independently H, C3-C6 alkyl or alkenyl; and pharmaceutically-suitable salts thereof; a synthetic method therefor, pharmaceutical dosage forms containing one of more of these compounds, and use of these compounds in the treatment of neoplastic cell growth, are disclosed.

Abstract: 1

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), (II) or (III), 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: 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.

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: Nobel polyamine compounds and polyamine compounds having carcinostatic action are provided. There are also provided anticancer agents containing as active ingredient at least one of polyamine compounds represented by the following Formula (I) or (III) and/or pharmaceutically acceptable salts thereof. Specifically, there are provided anticancer agents containing as active ingredient at least one of 1,18-bis(ethylamino)-5,14-diazaoctadecane, 1,16-bis(cyclopropylmethylamino)-5,12-diazahexadecane, 1,17-bis(cyclopropylmethylamino)-5,13-diazaheptadecane and/or pharmaceutically acceptable salts thereof.

Abstract: The present invention provides discrete-length polyethylene glycol and polyethylene glycol containing compounds and methods for their preparation.

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: A method for preventing adverse effects associated with the use of a medical device in a patient by introducing into the patient a device of which at least a portion includes a prophylactic or therapeutic amount of a nitric oxide adduct. The nitric oxide adduct can be present in a matrix coating on a surface of the medical device; can be coated per se on a surface of the medical device; can be directly or indirectly bound to reactive sites on a surface of the medical device; or at least a portion of the medical device can be formed of a material, such as a polymer, which includes the nitric oxide adduct. Also disclosed is a method for preventing adverse effects associated with the use of a medical device in a patient by introducing the device during a medical procedure and before or during said procedure locally administering a nitric oxide adduct to the site of contact of said device with any internal tissue.

Abstract: There is disclosed a class of pharmaceutical compositions useful for the treatment of cancer, particularly solid tumors, and having a mechanism of action as spermine antagonists. The present pharmaceutical compositions are able to inhibit the inhibitory effect of spermine upon macrophage function, and thus prevent spermine-induced immunosuppression.

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: An ascorbic acid-based composition and related method for the treatment of aging or photo-damaged skin is disclosed. The composition includes water and ascorbic acid, at least a portion of which has generally been pretreated by being dissolved under relatively high temperature and concentration conditions. The composition typically includes at least about 5.0% (w/v) ascorbic acid and may advantageously be formulated to have a pH above 3.5. Generally, the composition also includes non-toxic zinc salt, tyrosine compound, and/or pharmaceutically acceptable carrier. In addition, the composition may include an anti-inflammatory compound, such as aminosugar and/or sulfur-containing anti-inflammatory compound. The topical composition may be in the form of a serum, a hydrophilic lotion, an ointment, a cream, or a gel.

Abstract: Methods of identifying compounds that relax or stimulate arterial tension through their action on perivascular sensory nerve calcium receptors are described. Compounds identified through such methods are useful for the treatment of hypertension, hypotension and other diseases and conditions that alter normal physiological blood pressure.

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: Composition in the form of an aqueous solution, useful for disinfecting hard surfaces comprises: a) from 0.0005% to 20% by weight of peracetic acid, b) from 0.001% to 45% by weight of acetic acid, c) from 0.001% to 35% by weight of hydrogen peroxide, d) from 0.0001% to 2% by weight of at least one compound of formula (I) (R1) (R2) (R3)N→O  (I) e) if desired, up to 2.5% by weight of at least one nonionic surfactant, and wherein f) the weight ratio between the compound of formula (I) and the peracetic acid is less than or equal to 1, and in that g) the weight ratio between the nonionic surfactant and the peracetic acid is less than or equal to 0.2.

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 method of treatment for patients afflicted with malignant tumor cells in need of anti-neoplastic therapy, which cells are sensitive to a polyamine having one of the formulae: ##STR1## or (III) a salt thereof with a pharmaceutically acceptable acid comprising administering thereto an anti-neoplastic effective amount of the polyamine or salt thereof.

Abstract: This invention relates generally to medical treatment methods. Specifically, the invention relates to methodology for the correction of defective chloride transport by activation of chloride channels of the lung and other epithelia using genetic or chemical modification. These methods relate to the treatment of epithelia with compounds which cause activation of the channel as measured by increased probability (Po) of opening of the channel at physiologically relevant holding potentials. These methods also relate to the treatment of epithelia with gene therapy to introduce chloride channels genes with site mutations which cause activation of the channel as measured by increased probability (Po) of opening of the channel at physiologically relevant holding potentials. These treatments will reduce life-threatening complications frequently found in diseases such as cystic fibrosis. These methods of activation of chloride channels also comprise treatment of chloride channels with amidation reactions.

Abstract: A method for the treating septic shock in a patient comprises administering to the patient a therapeutically-effective amount of a composition comprising a compound having the formula (I): ##STR1## wherein R.sub.1 is hydrogen, hydroxyl, carboxyl, amino or C.sub.1 -C.sub.8 alkyl; R.sub.2 is hydrogen, hydroxyl, amino or C.sub.1 -C.sub.8 alkyl; and R.sub.3 is hydrogen, hydroxyl, carboxyl, amino, C.sub.1 -C.sub.8 alkyl, substituted or unsubstituted phenyl, amide, C.sub.3 -C.sub.8 aminoalkyl, or C.sub.1 -C.sub.8 aminoalkylcarbonyl; or a therapeutically-effective salt, ester or solvate thereof. Particularly preferred compounds for use in the present invention include butylamine, propylamine, diaminopropane, diaminobutanone, tyrosine, threonine, asparagine, and aspartate.

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: This invention relates to the treatment of pool surfaces and equipment with antimicrobial solutions which contain straight chain alkylamine compounds alone or in combination with additional bactericidal agents, such as biguanides.

Abstract: The present invention relates generally to a method for, and pharmaceutical compositions useful in, the prophylaxis and/or treatment of cardiac dysfunction in a mammal by the administration of an effective amount of an agent capable of blocking or inhibiting the effect or release of inositol(1,4,5)trisphosphate in cardiac tissue.

Abstract: 2,3,2 Tetramine (3,7-diazanonane-1,9-diamine) is propounded for the treatment of Parkinson's Disease and dementias characterized by mitochondrial damage in view of this compound's ability to completely neutralize the dopainine-depriving effect of MPTP in laboratory animals up to 12 hours post MPTP injection, and to retain partial protection at suboptimal tissue levels for up to 36 hours.