Abstract: Provided are compounds reducing SAICAR accumulation, and applications. On the basis of existing protein structure data and small molecule structure data, calculations and analysis are performed using software to screen and obtain compounds capable of effectively interfering with PAICS activity, reducing SAICAR synthesis, and ultimately reducing SAICAR accumulation, in order to achieve the goal of treating or improving ADSL deficiency. A better effect in the treatment or improvement of ADSL deficiency is expected from the joint use of at least two of the described compounds.

Abstract: Sanitizing cleaning/rinse aid compositions for various applications including institutional machine warewash sanitizing are disclosed. In particular, concentrated and use compositions, such as concentrated liquid rinse aid compositions or ware wash detergents, employing an amine-based surfactant and a defoaming agent are disclosed. In particular, the present disclosure provides compositions and methods for providing a sanitizing rinse with desired antimicrobial efficacy against a broad spectrum of gram-negative microbes, suitable foaming profiles, and beneficial applications of use of the same.

Abstract: The present invention provides methods for the regulation of osteopontin activity in a subject as well as for treating or preventing conditions associated with an increased activity of osteopontin activity in a subject.

Abstract: The present invention relates to a cosmetic or pharmaceutical composition for treating alopecia, and in general for counteracting excessive hair loss, comprising as an active ingredient a compound of formula (I) R—N1-spermidine, or 1,4-butane-diamine,N-(3-aminopropyl)-N1—R. The compounds of general formula (I) are active in accordance with the objects of the present invention, and also sufficiently stable to allow effective application for topical use on the scalp without potentially being transformed into a different substance, which is no longer active, as a result of oxidation.

Abstract: The disclosure relates to a novel use of a food composition for human use, having fewer than 1600 picomoles of polyamines, for the production of a medical food which is intended to combat a syndrome or pathology involving N-methyl-D-aspartate receptor subunit NR2-B.

Abstract: A composition for local application contains spermidine for the treatment of the stress urinary incontinence in a female subject. The composition is intended for transvaginal application to release spermidine onto external sphincter, urethra and endopelvic fascia, or for intravescial instillation. A variant composition takes the form of a condom lubricant comprising spermidine for the local release thereof during sexual intercourse, as an alternative or complementary to the local self-administration.

Abstract: A composition and method for treating infertility and sexual dysfunction of a male or female human by balancing hormone levels of cortisol, dehydroepiandrosterone sulfate, testosterone, progesterone, and estradiol in the human. The composition comprises effective amounts of spermine and spermidine, administered at least once daily for a period of at least thirty days.

Abstract: Campylobacter are the commonest reported bacterial causes of gastroenteritis in the UK and industrialized worlds. This invention relates to a method of preventing or reducing the colonisation of the gastrointestinal tract of an animal with Campylobacter. Accordingly, the present invention provides a method for disinfection of an animal comprising administering to said animal at least one compound that binds to MOMP or FlaA of Campylobacter in an effective amount to reduce the number of Campylobacter present in the gastrointestinal tract of said animal. The present invention also provides a method of preventing or reducing transmission of Campylobacter from one animal to another.

Abstract: Ion binding compounds and compositions may include compounds, polymers and compositions that include amine moieties. Ion binding polymers may be crosslinked amine polymers and may be used to remove ions, such as phosphate ions, from the gastrointestinal tract of animals, such as humans. Such compounds, polymers and compositions may be used therapeutically to treat a variety of medical conditions, such as hyperphosphatemia.

Abstract: A gynecologic composition contains spermidine to treat vulvar vestibulitis syndrome (VVS). In this therapeutic context, spermidine is effective at around one micromole per applied dose in the form of a simple salt or complex, alone or in combination or in conjunction with auxiliary actives such as anaesthetics and estrogens.

Abstract: The invention provides methods of immobilizing an active agent to a substrate surface, including the steps of, providing a substrate, contacting the substrate with a solution of a compound including a trihydroxyphenyl group, thereby forming a trihydroxyphenyl-treated substrate, and contacting the trihydroxyphenyl-treated substrate with an active agent, thereby immobilizing the active agent on the substrate. Further provided are methods of immobilizing an active agent on a substrate, including the steps of providing a substrate, combining a solution of a compound including a trihydroxyphenyl group with a solution of an active agent, thereby forming a solution of an active agent-trihydroxyphenyl conjugate, and contacting the substrate with the solution of the active agent-trihydroxyphenyl conjugate, thereby immobilizing the active agent on the substrate. The invention further provides substrates and medical device or device components with active agents immobilized on the surface thereof.

Abstract: Some embodiments of this invention include methods for treating disease and methods for administering a compound of the invention. In some aspects of the invention, diseases can be treated by administration of compositions comprising a compound of the invention. Pharmaceutical compositions of some embodiments of the present invention comprise a compound of the invention.

Abstract: The composition includes, per gram of composition, less than 600, in particular less than 400 picomoles of biologically active polyamines, for use in the prevention or treatment of radiotherapy-induced pathologies of the skin or mucous membranes in a patient, in particular a human or an animal.

Abstract: This invention relates to a composition, and methods of administration and treatment comprising a homeopathic preparation of an effective amount of Spermine and/or Spermidine that improves hormone imbalances in males and females. The purpose of the invention is to provide a homeopathic treatment comprising Spermine and/or Spermidine that demonstrates improvement in energy, sleep, sexual function, relief of prostrate symptoms, lighter and shorter hot flush symptoms, stamina, weight loss, and the overall mood and stress of a patient.

Abstract: Methods for preconditioning and/or providing neuroprotection to the animal central nervous system against the effects of cerebral hemorrhage and subarachnoid hemorrhage. Therapeutic agents are administered to the upper third of the nasal cavity to bypass the blood-brain barrier and access the central nervous system directly to avoid unwanted and potentially lethal side effects. Therapeutic agents include those substances that interact with iron and/or copper such as iron chelators, copper chelators, and antioxidants. A particular example of such therapeutic agents is the iron chelator deferoxamine (DFO). An effective amount of DFO may be administered to the upper third of the nasal cavity of a patient at risk for, or diagnosed with, cerebral hemorrhage and subarachnoid hemorrhage. The effective amount of DFO is delivered directly to the patient's central nervous system for preconditioning, preventing and/or treating the cerebral hemorrhage and subarachnoid hemorrhage.

Abstract: A composition and method for enhancing fertility of a male or female human by affecting levels of cortisol, dehydroepiandrosterone sulfate, testosterone, progesterone, and estradiol in the human. The composition comprises effective amounts of spermine and spermidine, administered at least once daily for a period of at least thirty days.

Abstract: A compound useful as a plant activator for activating an endogenous defense system of a plant to control disease damage is provided. A compound represented by the formula: (R3)NH—(CH2)4—N(R1)—(CH2)3—NH(R2) (one of R1 and R2 represents a linear C6-18 alkanoyl group or alkenoyl group, the other represents hydrogen atom or a protective group of amino group; and R3 represents hydrogen atom or a protective group of amino group).

Abstract: This invention regards the use of zeaxanthin and/or rutin, as such or further combined with spermidine, as the active principle in a pharmaceutical, dietary, or cosmetic composition, acting to inhibit caspase-3 and therefore to control apoptosis by preventing programmed cell death. The indication for this composition according to the invention is primarily the treatment of scalp disorders characterized by excessive cellular turnover including chemotherapy-induced alopecia, alopecia areata, androgenetic alopecia and telogen effluvium.

Abstract: The invention provides novel methods for maintaining eye health and ameliorating ophthalmic maladies in animals by administering to the animals an ophthalmic malady ameliorating amount of one or more polyamines. Generally, the polyamines are administered to the animals in amounts of from about 1 to about 200 mg/kg/day to ameliorate maladies such as cataracts and cloudy eye.

Abstract: Described are medicaments and methods of treating or preventing metabolic bone diseases, such as Critical Illness Related Metabolic Bone Disease or of critical illness induced Osteopenia secondary to ICU Admission by sufficient autophagy inducing compound to inhibit or suppress critical illness enhanced osteoclastogenesis or increased osteoclast differentiation. The methods include administering of an autophagy activating compound to a mammal to: treat or prevent a bone degenerative disorder; slow bone deterioration; restore lost bone; maintain bone mass and/or bone quality or inhibit bone resorption in particularly by inhibiting or reducing a process by which osteoclasts break down bone and release the minerals resulting in a transfer of calcium from bone fluid to the blood. Also described are methods for administering the autophagy activating compound to treat a bone disorder of hyperresorption of bone and/or enhanced activation of osteoclasts.

Abstract: Methods of treating or reducing biofilms, treating a biofilm-related disorder, and preventing biofilm formation using polyamines is described.

Abstract: This invention relates to a process of synthesis and composition of open chain (ring), closed ring, linear branched and or substituted polyamines, polyamine derived tyrosine phosphatase inhibitors and PPAR partial agonists/partial antagonists via a series of substitution reactions and optimizing the bioavailability and biological activities of the compounds. Polyamines prevent the toxicity of neurotoxins and diabetogenic toxins including paraquat, methyphenyl pyridine radical, rotenone, diazoxide, streptozotocin and alloxan.

Abstract: Methods of treating or reducing biofilms, treating a biofilm-related disorder, and preventing biofilm formation using polyamines is described.

Abstract: Methods and compositions for the effect of Cholesteryl ester transfer protein (CETP) polymorphisms on mRNA splicing, statin treatment outcome, response to CETP inhibitor drugs, and myocardial infarction risk are described.

Abstract: Methods and intermediates for synthesizing triethylenetetramine and salts thereof, as well as novel triethylenetetramine salts and their crystal structure, and triethylenetetramine salts of high purity.

Abstract: The present invention generally relates to polymers and macromolecules, in particular, to polymers useful in particles such as nanoparticles. One aspect of the invention is directed to a method of developing nanoparticles with desired properties. In one set of embodiments, the method includes producing libraries of nanoparticles having highly controlled properties, which can be formed by mixing together two or more macromolecules in different ratios. One or more of the macromolecules may be a polymeric conjugate of a moiety to a biocompatible polymer. In some cases, the nanoparticle may contain a drug. Other aspects of the invention are directed to methods using nanoparticle libraries.

Abstract: The present invention generally relates to polymers and macromolecules, in particular, to polymers useful in particles such as nanoparticles. One aspect of the invention is directed to a method of developing nanoparticles with desired properties. In one set of embodiments, the method includes producing libraries of nanoparticles having highly controlled properties, which can be formed by mixing together two or more macromolecules in different ratios. One or more of the macromolecules may be a polymeric conjugate of a moiety to a biocompatible polymer. In some cases, the nanoparticle may contain a drug. Other aspects of the invention are directed to methods using nanoparticle libraries.

Abstract: The present invention generally relates to polymers and macromolecules, in particular, to polymers useful in particles such as nanoparticles. One aspect of the invention is directed to a method of developing nanoparticles with desired properties. In one set of embodiments, the method includes producing libraries of nanoparticles having highly controlled properties, which can be formed by mixing together two or more macromolecules in different ratios. One or more of the macromolecules may be a polymeric conjugate of a moiety to a biocompatible polymer. In some cases, the nanoparticle may contain a drug. Other aspects of the invention are directed to methods using nanoparticle libraries.

Abstract: Supramolecular complexes are formed by polyanionic polymers and spermidine having a ratio of anionic equivalents raging from 101:1 to 107:1 eq/eq, more preferably from 102:1 to 104:1 eq/eq, whose components are linked by non-covalent, ionic interactions. The supramolecular complexes are exhibit high potency in eliciting fibroblast proliferation. Disclosed are medicinal/cosmetic compositions containing the supramolecular complexes for the trophism, maintenance, regeneration, and repair of connective tissues and mucosae in damaged or senescent conditions.

Abstract: The present invention relates to a method of modulating cellular activity. More particularly, the present invention provides a method of modulating apoptosis by modulating protein 14-3-3 phosphorylation and, thereby its functionality. The present invention still further extends to methods for identifying agents capable of modulating protein 14-3-3 phosphorylation. The method and molecules of the present invention are useful, inter alia, in the treatment and/or prophylaxis of conditions characterized by unwanted cellular activity, such as unwanted cell survival.

Abstract: A salt of a polyamine having the formula: with a pharmaceutically acceptable organic or inorganic acid, wherein at least one of the bridging groups ALK1, ALK2 and ALK3 contains at least one —CH(OH)-group which is not alpha- to any of the nitrogen atoms.

Abstract: Pharmaceutical compositions and methods for the treatment of subjects, including humans, who have or are at risk for various disease, disorders and conditions, including, mitochondria-associated diseases, disorders, and conditions, including respiratory chain disorders, and diseases, disorders and conditions associated with or characterized at least in part by mitochondria swelling, mitochondria dysfunction, mitochondria leaking, oxidative stress, increased mitochondria number, increased mitochondria and mitochondria-related protein mass, and increased mitochondria and related-related proteins expression.

Abstract: The invention provides a new use of a saturated amine compound, i.e., in manufacture of peripheral blood hematopoietic stem cell mobilizing agents. Experiments show that this compound (Code No. TA01) can efficiently mobilize hematopoietic stem cells into peripheral blood, and is a new type of hematopoietic stem cell mobilizing agents. The invention can play an important role in research and development of mobilizing agents for mobilizing hematopoietic stem cells into peripheral blood and has a promising application perspective.

Abstract: The present invention generally relates to polymers and macromolecules, in particular, to polymers useful in particles such as nanoparticles. One aspect of the invention is directed to a method of developing nanoparticles with desired properties. In one set of embodiments, the method includes producing libraries of nanoparticles having highly controlled properties, which can be formed by mixing together two or more macromolecules in different ratios. One or more of the macromolecules may be a polymeric conjugate of a moiety to a biocompatible polymer. In some cases, the nanoparticle may contain a drug. Other aspects of the invention are directed to methods using nanoparticle libraries.

Abstract: The present invention generally relates to polymers and macromolecules, in particular, to polymers useful in particles such as nanoparticles. One aspect of the invention is directed to a method of developing nanoparticles with desired properties. In one set of embodiments, the method includes producing libraries of nanoparticles having highly controlled properties, which can be formed by mixing together two or more macromolecules in different ratios. One or more of the macromolecules may be a polymeric conjugate of a moiety to a biocompatible polymer. In some cases, the nanoparticle may contain a drug. Other aspects of the invention are directed to methods using nanoparticle libraries.

Abstract: The present invention generally relates to polymers and macromolecules, in particular, to polymers useful in particles such as nanoparticles. One aspect of the invention is directed to a method of developing nanoparticles with desired properties. In one set of embodiments, the method includes producing libraries of nanoparticles having highly controlled properties, which can be formed by mixing together two or more macromolecules in different ratios. One or more of the macromolecules may be a polymeric conjugate of a moiety to a biocompatible polymer. In some cases, the nanoparticle may contain a drug. Other aspects of the invention are directed to methods using nanoparticle libraries.

Abstract: The present invention relates, in general, to pattern-recognition receptors (PRRs), including toll-like receptors (TLRs), and, in particular, to a method of inhibiting nucleic acid-induced activation of, for example, endosomal TLRs using an agent that binds to the nucleic acid (“nucleic acid binding agent”), preferably, in a manner that is independent of the nucleotide sequence, the chemistry (e.g., DNA or RNA, with or without base or sugar modifications) and/or the structure (e.g., double-stranded or single-stranded, complexed or uncomplexed with, for example protein) of the nucleic acid(s) responsible for inducing TLR activation. The invention also relates to methods of identifying nucleic acid binding agents suitable for use in such methods.

Abstract: The present invention, relates to methods including compounds, derivatives, antibodies, interfering RNA, biologies, polypeptides, dominant negative effectors, and their use in the treatment of neuropathic pain by inhibition of transient receptor potential (TRP) channels. In another embodiment, this invention relates to inhibitors, antagonists, and agonists of TRPC4. TRPC4 therapeutic agents and modulators include but are not limited to small molecule inhibitors, compounds, amino acid derivatives, polypeptides, RNA interference agents, natural chemicals, ligand derivatives, and ions. TRPC4 therapeutic agents and modulators are developed for the treatment of neuropathic pain, including but not limited to pain sensations such as nociception, hyperalgesia, allodynia, and loss of sensory function.

Abstract: Methods for modulating macrophage proliferation in an individual afflicted with or at risk for an ocular disease such as ARMD are provided. The methods employ a polyamine analog, or salt or protected derivative thereof. Macrophage proliferation has been implicated in a number of serious disorders, including ARMD. The invention also provides methods for aiding diagnosis and monitoring therapy of an ocular disease such as ARMD.

Abstract: Disclosed herein are methods for treating a disease involving ?-synucleic aggregation using (1) a compound which reduces the amount of polyamines in an amount effective to reduce ?-synucleic aggregation; (2) a compound which inhibits polyamine synthesis in an amount effective to reduce ?-synucleic aggregation; or (3) a compound which inhibits ?-synucleic aggregation in an amount effective to reduce ?-synucleic aggregation. Also disclosed are methods for reducing the amount of ?-synucleic aggregation in a brain cell using (1) a compound which reduces the amount of polyamines in an amount effective to reduce ?-synucleic aggregation; (2) a compound which inhibits polyamine synthesis in an amount effective to reduce ?-synucleic aggregation; or (3) a compound which inhibits ?-synucleic aggregation in an amount effective to reduce ?-synucleic aggregation. Disclosed herein are also compounds which can be used in the above described methods.

Abstract: The invention relates to the use of spermidine or a pharmaceutically acceptable derivative thereof as the active principle in a pharmaceutical, cosmetic or dietetic composition. The composition is used for promoting pigmentation of the hair, particularly the shaft of the hair. The invention also relates to the composition which promotes this pigmentation effect, the composition containing spermidine or a derivative thereof (such as a salt) as an active principle and is intended for topical or oral administration.

Abstract: The invention relates to the use of plasma membrane calcium ATPase (PMCA) inhibitors for inhibiting sperm mobility to achieve a contraceptive effect. The invention further relates to contraceptive agents comprising one or more PMCA inhibitors.

Abstract: The present invention is directed to compounds, combinations, compositions and methods for enhancing nitric oxide (NO) delivery to target sites, and in particular to muscle, both normal and dystrophic. Enhanced NO delivery according to the present invention may be achieved by using a combination of a muscle relaxant and an NO donor compound, or by using a compound of the invention: formula (I) wherein R1 is H, halo, C1-6 alkoxy or C1-6 alkyl; R2 is H, NO2 or C(O)NH2; R3 is H, NO2 or C(O)NH2; and at least one of R2 and R3 is NO2; or a pharmaceutically acceptable salt of the compound.

Abstract: The present invention relates to a method of treating a life threatening condition in a critically ill human patient with a non-infectuous disorder, wherein the critically ill patient is a patient receiving enteral or parenteral nutrition, the method comprising the step of administering to said patient an autophagy inducing agent.

Abstract: The present invention relates to defoaming compositions comprising compounds having the formula C5H11CH(CH2CH2CH3)CH2O(CH2CH(X)O)nH (I) where X=(CH2)aCH3 where a=0 or 1 and where n=0.5-5; and one or more hydrotropes selected from the group consisting of branched or linear C4-C10 alkyl glycosides and optionally one or more anionic hydrotrope selected from the group consisting of fatty acid soaps where the acyl group contains 10-22 carbon atoms, and which could be saturated or unsaturated, linear or branched; or a sulfonate chosen from the group cumene sulfonate and xylene sulfonate, and the use of such compositions as defoaming and/or antifoaming agents. The invention also pertains to a composition comprising a) a compound C5H11CH(CH2CH2CH3)CH2O(CH2CH(X)O)nH (I) where X=(CH2)aCH3 where a=0 or 1 and n=0.

Abstract: Topical compositions with a chaotrope are described. The compositions can comprise guanidinium chloride or a derivative thereof and an active, and they unexpectedly display rapid active delivery and improved active functionality upon application.

Abstract: This invention regards the use of zeaxanthin and/or rutin, as such or further combined with spermidine, as the active principle in a pharmaceutical, dietary, or cosmetic composition, acting to inhibit caspase-3 and therefore to control apoptosis by preventing programmed cell death. The indication for this composition according to the invention is primarily the treatment of scalp disorders characterized by excessive cellular turnover including chemotherapy-induced alopecia, alopecia areata, androgenetic alopecia and telogen effluvium.

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: Novel methods of treating a patient for diseases, disorders, and conditions including diabetes mellitus, comprising administering, for example, copper binding compounds.

Abstract: Methods for treating viral infections using polyamine analogs, including mitoguazone (MGBG), are provided. In these methods, polyamine analogs destroy macrophages that act as viral reservoirs, facilitating the destruction of the viruses that dwell within the macrophages. Examples of viral infections that may be treated with the present methods include, but are not limited to, infections from human immunodeficiency viruses. These methods differ from previous methods of treatment using polyamine analogs, wherein the polyamine analogs were administered only as anti-tumor agents.