Abstract: The present invention provides a process for producing an amino composition by addition reaction between a polyamine and an unsaturated hydrocarbon compound in the presence of a strongly basic alkali metal catalyst to obtain an amino composition containing not more than 2% by weight of unreacted polyamine and preferably not more than 10 ppm of alkali metal.

Abstract: The present invention provides methods and compositions for the treatment of ion imbalances. In particular, the invention provides polymeric and pharmaceutical compositions comprising crosslinked amine polymers. Methods of use of the polymeric and pharmaceutical compositions for therapeutic and/or prophylactic benefits are disclosed herein. Examples of these methods include the treatment of renal diseases and hyperphosphatemia.

Abstract: Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having the general structure: wherein Q is selected from the group consisting of N, O and S; L is any bivalent organic radical capable of linking each Q, such as C, CH, (CH2)l, or {(CH2)i-Y—(CH2)j}k, wherein Y is selected from the group consisting of CH2, an ether, a polyether, an amide, a polyamide, an ester, a sulfide, a urea, a thiourea, a guanidyl, a carbamoyl, a carbonate, a phosphate, a sulfate, a sulfoxide, an imine, a carbonyl, and a secondary amino group and wherein Y is optionally substituted by -X1-L?-X2-Z or -Z; R1-R6, independently of one another, are selected from the group consisting of H, —(CH2)p-D-Z, an alkyl, an alkenyl, an aryl, and an alkyl or alkyl ether optionally substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, a polyamide, an ester, a mercaptan, an alkylthio, a urea, a thiourea, a guanidyl, or a carbamoyl group, and

Abstract: The invention provides novel polyamine and amino thiol 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 or amino thiols formulated for topical or local delivery to epithelial or mucosal cells are disclosed. Methods of administering the pharmaceutical preparations are also disclosed.

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: Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having the general structure: wherein Q is selected from the group consisting of N, O and S; L is any bivalent organic radical capable of linking each Q, such as C, CH, (CH2)1, or {(CH2)i—Y—(CH2)j}k, wherein Y is selected from the group consisting of CH2, an ether, a polyether, an amide, a polyamide, an ester, a sulfide, a urea, a thiourea, a guanidyl, a carbamoyl, a carbonate, a phosphate, a sulfate, a sulfoxide, an imine, a carbonyl, and a secondary amino group and wherein Y is optionally substituted by —X1—L?—X2—Z or —Z; R1–R6, independently of one another, are selected from the group consisting of H, —CH2)p—D—Z, an alkyl, an alkenyl, an aryl, and an alkyl or alkyl ether optionally substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, a polyamide, an ester, a mercaptan, an alkylthio, a urea, a thiourea, a guanidyl, or a carbamoyl group, and

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 in the cell, functio

Abstract: A purification method is disclosed for a predetermined water-insoluble extractant present in a liquid phase composition that additionally contains one or more additional extractants, synthesis reaction starting materials, and reaction byproducts dissolved as solutes in an organic diluent. An ion-containing compound is admixed with the composition to form an extractant/ion complex in the organic diluent phase that has an affinity for a new phase that is greater than the affinity for the first-named phase. The predetermined extractant/ion complex is separated from the diluent by using the new phase affinity, and the extractant/ion complex is preferably although not necessarily recovered. The extractant/ion complex is separated into extractant and ion. The extractant is recovered. Exemplary extractants include polyethers, crown ethers, crown thioethers, calixarenes, polyamines, cryptands, porphyrins and the like.

Abstract: Carboxylic acid-substituted polyalkylene polyamines in which amine nitrogen atoms on the polyamine backbone structure are replaced by guanidine groups provide a pH range extending into high pH values. These substances are useful as carrier ampholytes in isoelectric focusing.

Abstract: The present invention relates to synthetic cationic lipids, liposome formulations and the use of such compounds to introduce functional bioactive agents into cultured cells.

Abstract: The present invention describes the design, synthesis and therapeutic use of a variety of novel inhibitors of polyamine transport. The main feature of this class of transport inhibitors is to incorporate a linker or side chain that prevents the uptake of polyamines and helps to conjugate polyamine analogs to form dimers with high inhibitory potency against polyamine uptake. These new compounds incorporate features that are designed to maximize their chemical and metabolic stability and their ability to bind to the polyamine transporter, and to minimize their toxicity by preventing their absorption by the cells. The purpose of such inhibitors is to prevent the uptake or salvaging of circulating polyamines by rapidly proliferating cells such as tumor cells, in order to potentiate the effect of therapeutic inhibitors of polyamine biosynthesis such as alpha-difluoromethylornithene.

Abstract: The synthesis and use of a novel class of tumor necrosis factor (TNF?) inhibitors and immunomodulators are provided. These compounds have pharmacological applications as well as uses in assays relating to TNF? and other involved cytokines. As pharmaceuticals, these compounds are used to treat inflammatory, infectious, autoimmune or other proliferative diseases and conditions related to the unwanted presence or activity of TNF? and/or one or more other involved cytokines, alone or in combination with other agents.

Abstract: When the reaction solution formed during the addition of an alkylene oxide to an active hydrogen-containing compound has viscosity of not less than 10 mPa·s, this invention provides a method for stirring the reaction solution by the rotation of a vane or vanes continuously disposed in the vertical direction within an agitating reaction vessel in such a manner that the numerical value C represented by the following formula (1): C=A/(h2−h1)  (1) (wherein A denotes the length (m) of the vane or the vanes newly immersed by the supply of alkylene oxide, h1 denotes the height (m) of the liquid level before the supply of alkylene oxide, and h2 denotes the height (m) of the liquid level after the supply of alkylene oxide) may be not less than 0.5. By employing the method of this invention, it is made possible to effect addition of an alkylene oxide to the active hydrogen-containing compound with high efficiency.

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: A polyamine having the formula: H2N—A[NR—B]aNH2 or salt thereof, wherein A and B, which may be the same or different, are selected from aliphatic or aromatic substituents provided that at least four carbon atoms separate any two nitrogen groups, R is an aliphatic or aromatic group, and a is 2 to 5. In addition, a polymer having the formula: or salt thereof, wherein A, B and Q, which may be the same or different, are selected from aliphatic or aromatic substituents provided that at least four carbon atoms separate any two nitrogen groups, R is an aliphatic or aromatic group, a is greater than 1 to about 5, and n is 3 to about 1,000. The polymers are useful for improving acid-dyeability of polymer compositions, fibers, fabrics, films and other articles.

Abstract: Primers for cyanoacrylate adhesives which are based on compounds having multiple amine groups thereon (“multi-amines”) which have at least three secondary or tertiary amine groups, at least one of which is a tertiary amine group. The multi-amine compounds are characterized by having thereon at least three terminal and/or pendant aliphatic hydrocarbon groups of at least 4 carbon atoms in length. Such primers give substantially improved bond strengths to cyanoacrylate adhesive bonded assemblies comprising a polyolefin substrate such as high density polyethylene, LDPE or polypropylene. The multi-amine may have a cascade, dendrimer, hyperbranched or comb-like structure.

Abstract: The present invention provides an amine or polyamine, which has a surface activity not inferior to a solid tallow-based amine and an excellent workability. A salt of the amine is suited for emulsifying asphalt and the like, and also provides an asphalt emulsion composition which is obtained by using the salt and which has a quick setting property. Namely, the prevent invention provides a polyamine represented by the formula (1), a process for producing the amine, and an asphalt emulsion composition containing a water-soluble salt of the amine. wherein R is a straight or branched hydrocarbon group having 8 to 22 carbon atoms; x is a number of 1 to 5; and each of y and z is a number of 0 to 5 with the proviso that both of y and z are not 0 at the same time.

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: 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: 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: 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: Polyamines having the formula: 1

Abstract: An RNA polymerase transcription accelerator comprising a compound represented by the following Formula (I) or salts thereof.

Abstract: A polyamine having the formula:

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: 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: Polyamines having the formula: 1

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: Ethyleneamine compound(s), or mixtures thereof, are used in effective amounts to reduce or inhibit the deposition of white pitch on the paper making equipment during the processing to recycle coated paper.

Abstract: This invention relates to a composition containing (a) a component selected from the group of a mono- or poly- vinyl substituted mono- or poly-ether, a mono- or poly- vinyl substituted lactam, or a mixture thereof contained in an acidic medium and (b) an aliphatic, primary or secondary mono- or poly-amine at a concentration sufficient to adjust the pH of the composition above

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: 1

Abstract: Polyamines having the formula: 1

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: The present invention relates to new lipopolyamines (including salts thereof) characterised by a symmetrical, highly flexible lipophilic moiety having buffering capacity at physiological pH, and to the use thereof for the in vivo or in vitro introduction of biologically active materials, such as, for example, DNA, RNA, ribozymes, antisense DNA, PNA, peptides and proteins, into eukaryotic cells.

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: Disclosed are processes for the preparation of compounds of the formula (I): H2N—(CH2)n—A—(CH2)m—NH2, or (II): H2N—(CH2)n—NH—C(═NR1)—NH—(CH2)m—NH2, wherein n and m are each independently an integer from 2 to 8; A is selected from the group consisting of —NR1—, —NR1—(CH2)r—NR1— and —NR1—(CH2)r—NR1—(CH2)z—NR1—, wherein r and z are an integer ranging from 2 to 8; and R1 is hydrogen or a protecting group having a carbonyl group.

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: 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 provides a process of transfecting a cell with a polynucleotide mixed with one or more amphipathic compounds and an effective amount of a DNA-binding protein. Exemplary and preferred DNA-binding proteins are H1, H2A, and H2B. Exemplary and preferred amphipathic compounds are cationic amphipathic compounds.

Abstract: A compound having the formula: ##STR1## wherein: R.sub.1 -R.sub.6 may be the same or different and are H, alkyl or aralkyl having from1 to 12 carbon atoms;m is an integer from 3 to 6, inclusive;n is an integer from 3 to 6, inclusive;excluding those compounds of formula (I) wherein all of R.sub.1 -R.sub.6 are H and further excluding those compounds of formula (I) wherein:1) m is 3, n is 4, R.sub.1, R.sub.2, R.sub.5 and R.sub.6 are all H, and R.sub.3 and R.sub.4 are methyl;2) m is 3, n is 4, R.sub.1 and R.sub.6 are methyl or ethyl, and R.sub.2 -R.sub.5 are all H;3) m is 3, n is 4, and R.sub.1 -R.sub.6 are all methyl, ethyl or propyl;4) m and n are 3, R.sub.1, R.sub.2, R.sub.5 and R.sub.6 are all H, and R.sub.3 and R.sub.4 are methyl;5) m and n are 3 and R.sub.1 -R.sub.6 are all methyl;6) m and n are 3, R.sub.1 and R.sub.6 are H, and R.sub.2 -R.sub.5 are all methyl;7) m and n are 3, R.sub.1 and R.sub.6 are methyl, and R.sub.2 -R.sub.5 are all H;8) m and n are 3, R.sub.1 and are R.sub.6 are hydrogen, R.sub.

Abstract: The present invention provides improved adhesion promoters for latex paints. The adhesion promoters are enamines of acetoacetate esters, or substituted acetoacetate esters. The invention also provides two new compounds which are useful as adhesion promoters: 2-butyl-2-ethyl-1,3-propanediol bis(3-amino-2-butenoate) and trimethyl propane tris(3-amino-2-butenoate), and which are stable to hydrolysis on prolonged storage.

Abstract: The present invention relates to an amination process for the manufacture of polyamines. The purpose of the process is to increase the selectivity of linear aminated products and to prevent the formation of discoloring by-products or by-products which may later cause discoloration. According to the process this is achieved by performing, in a first part of the process, the amination to a conversion degree of between 50 and 98% by weight, calculated on the total yield of polyamines, at a proportionally time-weighted average temperature, which is at least 15.degree. C. higher than the proportionally time-weighted average temperature in the remaining part.

Abstract: Reaction products of polymers of C.sub.2 -C.sub.6 -olefins having an average degree of polymerization P of from 5 to 100 and oxides of nitrogen or mixtures of oxides of nitrogen and oxygen are used as additives for fuels, in particular for fuels for gasoline engines.

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.