Abstract: The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.

Abstract: The present invention relates to a cationic lipid having one or more biodegradable groups located in the mid- or distal section of a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.

Abstract: Methods of retarding formation of a lipofuscin pigment in the retina and of treating or ameliorating the effects of a disease characterized by an accumulation of a lipofuscin pigment in a retina are provided. These methods include the step of administering to a patient in need thereof a substituted C20-retinoid in an amount sufficient to reduce accumulation of a lipofuscin pigment in the retina. Further provided are methods of retarding formation of A2E and/or ATR-dimer by replacing an all-frans-retinal (ATR) substrate with a C20-D3-retinal substrate under conditions sufficient to impede the formation of A2E. Compositions for retarding formation of a lipofuscin pigment in the retina containing a substituted C20-retinoid and a pharmaceutically acceptable carrier are also provided.

Abstract: The invention relates to a purified Isometheptene compound comprising the structure according to Formula (I), or a hydrochloride, or a pharmaceutically acceptable addition salt thereof. In particular, the disclosure relates to the synthesis, purification and characterization of an Isometheptene isomer mucate crystal 2, wherein the Isometheptene isomer 2 is stereochemically characterized as (R)-enantiomer, respectively. The Isometheptene (R)-enantiomer activity indicates a selective centrally acting selective ligand for Imidazoline subtype 1 (I1) receptor sites; and more specifically, the disclosure provides an antihypertensive composition for treatment of migraine and other neurovascular or neurogenic pain from abdominal distress. (R)-Isometheptene enantiomer or isomer 2 may be an anti-hypertensive agent with lower side effects than the racemate form. Therefore (R)-Isometheptene is believed to be effective against episodic tension-type headaches (ETTH).

Abstract: N1,N4-bis(buta-1,3-dienyl)butane-1,4-diamine dihydrochloride (also referred to as MDL 72,527 and N,N?-di-2,3-butadienyl-1,4-butanediamine dihydrochloride), or salts or solvates thereof, its use as an antioxidant, its use in preventing and/or treating prostate cancer in male humans, and its use in reducing the concentration of reactive oxygen species in human prostate gland tissue or any other body tissue, and methods of making the compound thereof are disclosed. Other disclosed methods include inhibiting acetyl polyamine oxidase in human prostate tissue or other human body tissue comprising administering a therapeutic amount of N,N?-bis(2,3-butadienyl)-1,4-butanediamine or a salt or solvate thereof to the human, and a method of determining oxidative stress in human prostate tissue or other human or animal body tissue comprising measuring a ratio of oxidized 2?,7?-dichlorodihydrofluorescein diacetate fluorescence:DNA fluorescence and hydroethidine dye fluorescence ex vivo or in vivo.

Abstract: The present invention relates to the use of polyaminoisoprenyl derivatives in antibiotic or antiseptic treatment of bacteria including those presenting multiple drug resistance (MDR), in particular as efflux pump inhibitors. It also relates to novel polyaminoisoprenyl derivatives, compositions comprising the same, process for preparing the same, and use thereof in antibiotic or antiseptic treatment.

Abstract: The present application provides a terpene analogue of Formula (I) or a pharmaceutically acceptable isomer, salt or ester thereof, and methods and uses thereof for treating neurological conditions such as pain in general and neuropathic pain. These terpene analogues can also be used to treat other electrical disorders in the central and peripheral nervous system. Also provided are methods of synthesizing the terpene analogues of Formula I.

Abstract: Combination methods for treatment of cancer and of blood disorders, using PG-11047 ((2Z)-N1,N4-bis[3-(ethy-lammo) propyl]-2-butene-1,4-diamine) and PG-11048 ((2E)-N1,N4-bis[3-(ethylamino)propyl]-2-butene-1,4-diamine) in combination with DNA methyltransferase (DNMT) inhibitors, histone deacetylase (HDAC) inhibitors, or both DNA methyltransferase inhibitors and histone deacetylase inhibitors, are disclosed. Hematopoietic cancers, lung cancers, mesothelioma, cutaneous T-cell lymphoma (CTCL), multiple myeloma, solid tumors, and blood disorders such as myelodysplastic syndromes can be treated using the methods of the invention.

Abstract: The present invention provides for the treatment or prevention of Hepadnaviridae infection and disease caused by Hepadnaviridae infection. In particular, the invention provides compositions and methods that affect the ability of Hepadnaviridae to utilize the host's cellular machinery as part of the virus' lifecycle. The invention relates to the discovery that interfering with the normal ability of viruses to utilize the host cell machinery with LSD1 inhibitors reduces HBV replication. Thus, the treatment and prevention of Hepadnaviridae infection and disease caused by Hepadnaviridae according to the invention comprises administering to an individual in need of treatment, a therapeutically effective amount of a LSD1 inhibitor. The individual in need of treatment can be a human or, e.g., another mammal.

Abstract: The present invention provides various pharmaceutical compositions, in particular for oral administration, formulated for extended release of active compounds useful in the treatment of neurodegenerative diseases, in particular Parkinson's disease, and injuries to the nervous system. The active compound comprised within these compositions is preferably selected from N-propargyl-1-aminoindan, an enantiomer thereof, or a pharmaceutically acceptable salt thereof, more preferably rasagiline or a pharmaceutically acceptable salt thereof.

Abstract: Described are methods of improving insulin sensitivity, and treating fatty liver disease (including non-alcoholic steatohepatitis (NASH)), by administering specific inhibitors of PKC delta.

Abstract: Methods for stabilizing ?-galactosidase, stabilizing ?-glucocerebrosidase, treating a glycolipid metabolic disorder caused by mutation of ?-galactosidase gene, treating a glycolipid metabolic disorder caused by mutation of ?-glucocerebrosidase gene, regenerating the activity of ?-galactosidase, regenerating the activity of ?-glucosidase, treating GM1 gangliosidosis, Morquio-B or Krabbe's disease, and treating Gaucher's disease, include administering a carba-sugar amine derivative represented by the following formula (1) or (2):

Abstract: The present invention relates to the use of an antifungal agent or of a compound capable of binding to a mannoprotein and blocking the binding of said mannoprotein to an endothelial cell receptor, in the preparation of a pharmaceutical composition for treating a disease associated to an unwanted cell adhesion. Likewise, the present invention also contemplates methods aimed at identifying a compound potentially useful for preventing and/or treating a disease associated to an unwanted cell adhesion, for predicting the probability of a patient suffering from cancer to suffer from metastasis and for designing a personalized therapy for a patient suffering from cancer.

Abstract: Provided herein are methods of treating obesity and diabetes with labile bile acid sequestrants. An effective amount of a labile bile acid sequestrant may be orally administered to an obese or diabetic individual. A labile bile acid sequestrant provided herein may have a low affinity in the colon or rectum of a human for at least one bile acid or bile acid mimic that stimulates L-cells. A labile bile acid sequestrant may be a non-systemic labile bile acid sequestrant.

Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.

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.

Abstract: Methods of retarding formation of a lipofuscin pigment in the retina and of treating or ameliorating the effects of a disease characterized by an accumulation of a lipofuscin pigment in a retina are provided. These methods include the step of administering to a patient in need thereof a substituted C20-retinoid in an amount sufficient to reduce accumulation of a lipofuscin pigment in the retina. Further provided are methods of retarding formation of A2E and/or ATR-dimer by replacing an all-frans-retinal (ATR) substrate with a C20-D3-retinal substrate under conditions sufficient to impede the formation of A2E. Compositions for retarding formation of a lipofuscin pigment in the retina containing a substituted C20-retinoid and a pharmaceutically acceptable carrier are also provided.

Abstract: The use of bis-amines to enhance the antimicrobial activity of pharmaceutical compositions is described. The bis-amines are particularly useful for enhancing the antimicrobial activity of aqueous ophthalmic compositions, such as artificial tears or ocular lubricants, and solutions for disinfecting contact lenses.

Abstract: The present disclosure generally relates to a multi-component biocide composition comprising a borate component in combination with an azole component to both inhibit mold fungi, decay fungi, such as brown-rot fungi and white-rot fungi, and to resist insect infestation.

Abstract: A polyamine-depleted food compositions is provided for preparing foods, intended for humans or animals, for preventing or treating heart rate anomalies.

Abstract: The application is based on the observation that tumor stem cell (TSC) replication involves a replicative intermediate configuration wherein a substantial fraction of the TSC genome is present as single-stranded DNA (ssDNA) when bell-shaped nuclei commence separation into two nuclei. During this replicative intermediate configuration large amounts of ssDNA are thus present in the nuclei of cells which the applicant proposes as target for anti-tumor therapy. A method of screening for anti-tumorigenic agents targeting ssDNA and use of such agents in therapy is claimed.

Abstract: A carba-sugar amine derivative represented by the following formula (1) or (2) is used as the active ingredient of a ?-galactosidase inhibitor or a glycolipid metabolic disorder treating agent. Wherein each of R1 and R2 independently represents H, an alkyl group, an acyl group, an aryl group or an aralkyl group, with the proviso that both are not H at the same time, and each of R3, R4, R5 and R6 independently represents a hydroxyl group or hydroxyl group having a substituent. Also, R7 represents an alkyl group, and each of R8, R9, R10 and R11 independently represents a hydroxyl group or a hydroxyl group having a substituent.

Abstract: The invention relates to the use of C10-C14-alkane-1,2-diols, in particular 1,2-decanediol, 1,2-dodecanediol and/or 1,2-tetradecanediol, in the preparation of a composition for the prophylaxis and/or treatment of Malassezia-induced dandruff formation, as well as to cosmetic and/or dermatological preparations comprising C10-C14-alkane-1,2-diols.

Abstract: A tropical composition is provided. The topical composition can be prepared by diluting a topical composition precursor with water and adding additional components, if desired. The topical composition precursor can be prepared by melt processing a hydrophobic polymer composition that includes repeating pyrrolidone/alkylene groups wherein the alkylene groups contain at least 10 carbon atoms, and a hydrophilic polymer composition including repeating carboxylic groups and/or repeating hydroxyl groups. A topical composition precursor and methods for manufacturing and using a topical composition are provided by the invention.

Abstract: Disclosed are a water-soluble metal-processing agent and a coolant both of which have excellent microbial deterioration resistance and are less likely to go rotten, a method for preparing the agent or the coolant, and a metal processing method. The water-soluble metal-processing agent or the coolant comprises an N,N,N?,N?-tetraalkyldiamine compound. The metal processing method is characterized by processing a metal of interest by using the water-soluble metal-processing agent or the coolant.

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 present invention relates to methods for treating and completely curing fungal, yeast and/or mold infections in human subjects comprising topically administering to a human subject in need thereof an antifungal nanoemulsion composition.

Abstract: The application discloses metallized chelator complexes and uses of metallized chelator complexes for dissolving ?-sheet proteins and reducing formation of ?-sheet proteins, where the metallized chelator complex comprises a metal ion chelator and a metal ion.

Abstract: Provided herein are compositions and methods for treating ophthalmic diseases and disorders. Compositions comprising retinylamine derivative compounds provided herein are useful for treating and preventing ophthalmic diseases and disorders, including diabetic retinopathy diabetic maculopathy, diabetic macular edema, retinal ischemia, ischemia-reperfusion related retinal injury, and metabolic optic neuropathy.

Abstract: Particular aspects of the present invention provide pharmaceutical compositions comprising isoprenoid-based compounds (e.g., farnesol and/or farnesol analogues or derivatives) or dehydroisoprenoid-based compounds, and novel methods for using same in treating (e.g., suppressing): alcohol withdrawal syndrome and associated neurological symptoms (e.g., depression, tremor, anxiety, autonomic hyperactivity (e.g., sweating, increased blood pressure, tachycardia), hallucinations, alcohol withdrawal seizures, delirium tremens (DT), and memory loss); or for treating in treating convulsive seizure (e.g., epileptic seizure, etc.).

Abstract: The use of bis-amines to enhance the antimicrobial activity of pharmaceutical compositions is described. The bis-amines are particularly useful for enhancing the antimicrobial activity of aqueous ophthalmic compositions, such as artificial tears or ocular lubricants, and solutions for disinfecting contact lenses.

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 invention is an increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages. The allylamine active ingredient is prepared in an acidic environment; the acidic environment altering the physiochemical properties of the active ingredient resulting in the active ingredient having a positive charge. The positive charge and enhancers used in the formula allow for increased penetration of the active ingredient through skin and skin appendages. The positively charged active ingredients are either dissolved in the vehicle directly or dissolved in a plurality of beads suspended in the vehicle.

Abstract: A method for the treatment of acne comprising the administration, to a patient afflicted therewith, of a effective amount of a squalene monooxygenase inhibitor such as tolnaftate, naftifine, terbinafine, butenafine or ciclopirox. An advantage of the present invention relates to the surprisingly speedy onset of effectiveness in relieving acne symptoms. The compound may be administered orally or topically.

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: The present application relates to the use of active compound combinations containing phenolic active compounds and fungicidal active compounds for preserving animal hides and leather.

Abstract: A chemical composition and method of use of the composition is described. The chemical composition includes an aza-enediynes, aza-enyne allenes, or an aza-diallenes. These compound are preferably non-hydrolyzable, cationic compounds that bind to nucleic acids. In addition it is believed that these compounds may undergo chemical reactions in the presence of a nucleic acid to generate reactive intermediates that cleave nucleic acids.

Abstract: Disclosed is both a method and composition for controlling deleterious organisms, such as insects, nematodes and weeds while maintaining beneficial soil organisms, by applying a compound comprised of a liquid medium and comprising an azide and an amino acid polymer. The azide can be selected from the group consisting of sodium azide and potassium azide or a combination of the two. The composition provides an effective pesticide, without causing significant harm to the environment. The composition may be applied to soil to control a population of a deleterious organism.

Abstract: Described in the present invention are a dispersion which comprises, as a dispersoid, (a) 5 to 40 wt. % of an amphipatic lipid containing, in the molecule thereof, at least one hydroxy and amide group, and (b) 2 to 55 wt. % of a surfactant in an aqueous medium; a washing-away type cosmetic composition comprising the dispersion; and a washing-away type cosmetic composition comprising (A) 0.01 to 10 wt. % of an amphipatic lipid which contains, in the molecule thereof, at least one hydroxy and amide group and having a melting point not less than 30° C. and (B) 5 to 95 wt. % of a surfactant. The dispersion according to the present invention is useful as a component of a washing-away type cosmetic composition having both an emulsion-like or pearl-lustrous appearance and low skin irritation.

Abstract: Novel conformationally restricted polyamine analogs are provided, as well as compositions comprising these novel polyamine analogs. Methods of using the novel polyamine analogs in treatment of diseases such as cancer are also provided. Also provided is a method of delivering these analogs specifically to tumor cells by covalently attaching polyamine analogs to porphyrin compounds, along with novel polyamine-porphyrin covalent conjugates.

Abstract: Antineoplastic drug modulators are described. The specific modulators referred to are propargylamines which can enhance the cytotoxic effects of antineoplastic drugs on cancer cells while protecting normal cells from damage. The propargylamine modulators can be used to increase the selectivity and effectiveness of conventional antineoplastic drugs, to reduce the unwanted side-effects of cancer chemotherapy, to improve effectiveness of cancer chemotherapy, to improve treatment of cancers for which treatment is otherwise ineffective, to improve therapy of cancers otherwise unresponsive or poorly responsive due to drug-resistance and/or toxicity limited treatment regimens and to render effective chemotherapy for previously untreatable cancers.

Abstract: Novel conformationally restricted polyamine analogs are provided, as well as compositions comprising these novel polyamine analogs. Methods of using the novel polyamine analogs in treatment of diseases such as cancer are also provided. Also provided is a method of delivering these analogs specifically to tumor cells by covalently attaching polyamine analogs to, porphyrin compounds, along with novel polyamine-porphyrin covalent conjugates.

Abstract: The present invention relates to a method for treating or preventing bone fracture, which comprises administering an effective amount of calcium L-threonate to a subject in need of such prevention or treatment. It had been found from experiments that calcium L-threonate could not only promote proliferation, differentiation and mineralization of osteoblasts, but also could promote the expression of collagen I mRNA of osteoblasts cultured in vitro. Accordingly it facilitated bone fracture healing and increased bone density and mechanical performance, so as to prevent or treat bone fracture.

Abstract: The present invention relates to a method for preventing or treating of cartilage related diseases, such as osteoarthritis, rheumatoid arthritis, articular cartilage damage, multiple chondritis, osteochondrosis, etc., which comprises administering an effective amount of calcium L-threonate to a subject in need of such prevention or treatment. It had been demonstrated by experiments that calcium L-threonate could improve significantly the positive expression percentage of collagen I mRNA in the chondrocyte and osteoblast, improved significantly the positive expression percentage of articular cartilage and epiphyseal cartilage, facilitated the growth of chondrocyte, increased the quantity of bone collagen, and promoted the formation of bone and cartilage matrix and the synthesis of proteoglycan. It could also promote the formation of bone nourishing blood vessels and improve the microcirculation of bone.

Abstract: A chemical composition and method of use of the composition is described. The chemical composition includes an aza-enediyne, aza-enyne allene, or an aza-diallene. These compound are preferably non-hydrolyzable, cationic compounds that bind to nucleic acids. In addition it is believed that these compounds may undergo chemical reactions in the presence of a nucleic acid to generate reactive intermediates that cleave nucleic acids.

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: 20-HETE agonists and antagonists are disclosed along with therapeutic applications. In a preferable form of the invention, the 20-HETE agonists are selected from the group consisting of 21-hydroxyheneicosa-5(Z), 8(Z), 11(Z), 14(Z)-tetraenoic acid, 20-hydroxyeicosa-5(Z), 14(Z)-dienoic acid and 20-, 21-dimethyl 20-HETE. Preferable 20-HETE antagonists include 5(S)-HETE, 15(S)-HETE, 19(S)-HETE, 19-hydroxynonadeca-5(Z), 8(Z), 11(Z), 14(Z)-tetraenoic acid and 20-hydroxyeicosa 6(Z), 15(Z)-dienoic acid.

Abstract: A non-toxic, environmentally safe and easily employable insecticide and insect repellent is achieved by providing an aqueous composition incorporating ethanolamine based compounds, either independently or in combination with the ethanolamine based compounds being selected from both simple compounds and conjugated compounds. In one preferred embodiment, a highly effective composition is attained for safe, effective, direct topical application to humans and animals by employing between about 10% and 70% by volume of the entire composition of the ethanolamine-based compound. In alternate preferred embodiments, the insecticide is formulated for application to plants, trees, crops, and other vegetation to provide a composition which effectively controls bothersome insects, while being completely safe and non-injurious to the plant, tree, or crop, as well as to the flowers or fruit thereof.

Abstract: 20-HETE agonists and antagonists are disclosed along with therapeutic applications. In a preferable form of the invention, the 20-HETE agonists are selected from the group consisting of 21-hydroxyheneicosa-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid, 20-hydroxyeicosa-5(Z),4(Z)-dienoic acid and 20-,21-dimethyl 20-HETE. Preferable 20-HETE antagonists include 5(S)-HETE, 15(S)-HETE, 19(S)-HETE, 19-hydroxynonadeca-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid and 20-hydroxyeicosa 6(Z),15(Z)-dienoic acid.

Abstract: Disclosed is a dermal barrier composition which contains a hydrophilic polymer emulsion and a hydrophobic polymer emulsion. The dermal barrier composition is moisture activated, and remains inert until the hydrophobic and hydrophilic polymer emulsions contact a suitable substrate such as human skin. The dermal barrier composition is itself an emulsion, and can optionally contain a biocidal agent for antimicrobial and antiviral efficacy. The dermal barrier composition can also contain other active agents such as sunscreens, insect repellents and fungicides. The dermal barrier composition can be applied topically to skin, where it forms a protective or barrier layer against a number of pathogenic and chemical irritants.