Abstract: The present invention provides topical compositions, methods of preparation, and methods of treatment for onychomychosis. In certain specific embodiments, the invention provides an anti-fungal pharmaceutical composition for topical application comprising an anti-fungal agent, a zwitterionic surfactant or charged derivative thereof; a carboxylic acid, a lower alcohol, and water. The acid is selected from a short-chain hydroxy acid, a short-chain fatty acid, and a mixture thereof. In certain other specific embodiments, the invention provides an anti-fungal pharmaceutical composition for topical application comprising an anti-fungal agent, a quarternary amino acid, a keratolytic agent; a lower alcohol; and water. In certain embodiments, the keratolytic agent is urea, ammonium thioglycolate, or a mixture thereof.

Abstract: A pharmaceutical composition is described which includes: an antifungal agent from the class of the allylamines or the morpholines, at a concentration of at least 5%; a ternary solvent system comprising water; at least one branched or straight chain C2-C8 alkanol; at least one glycol; the total amount of water representing more than 30% (w/w) of the composition. This composition is intended for application to the nail for the treatment of onychomycoses.

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: The present invention provides an adhesive patch for the treatment of tinea unguium intended to be applied once a day, comprising terbinafine and/or a pharmacologically acceptable salt thereof in an amount of 3 mg/cm2, wherein the adhesive patch is used so that the terbinafine concentration in nails may be 295±127 ng/mg and the terbinafine concentration in plasma may be 23 pg/mL or less, 8 weeks after the start of application, per cm2 of the patch size.

Abstract: The present invention relates to the compounds of formula I, processes for their production and their use as anti-inflammatory agents.

Abstract: The subject matter of the present invention is novel families of compounds which are aromatic amine, imine, aminoadamantane and benzodiazepine derivatives, medicaments comprising same and the use thereof as inhibitors of the toxic effects of toxins with intracellular activity, such as, for example, ricin, and of viruses that use the internalization pathway for infecting cells.

Abstract: Methods of treating exposure to Giardia lamblia and/or giardiasis and methods of antagonizing Giardia lamblia attachment to the intestinal wall of a subject are described herein.

Abstract: The present invention relates to a method of disinfecting a surface and to antimicrobial composition, particularly for personal cleaning, oral care, or hard surface cleaning. It is an object of the present invention to provide for an antimicrobial composition that has relatively fast antimicrobial action. The inventors have found that use of small amounts of eugenol in combination with thymol and terpineol enables this fast kinetics at much lower amount of thymol and terpineol than without eugenol.

Abstract: A pharmaceutical composition comprises a solid amorphous dispersion of a cholesteryl ester transfer protein inhibitor and a concentration-enhancing polymer.

Abstract: Provided are a triterpene derivative represented by a general formula (I), a pharmaceutically acceptable salt thereof, and an agent for preventing or treating chronic hepatitis C comprising the triterpene derivative or the salt as an active ingredient: [in the formula (I), R1 represents a carboxyl group, a hydroxymethyl group, —CH2OSO3H, or and R2 represents —OR3 or —O— (CH2) m-OR4, where R3 represents a benzyl group which may be substituted with a hydroxymethyl group, a dimethylaminomethyl group, a phenylaminomethyl group, a morpholinomethyl group, a carboxyl group, or a formyl group, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, or a hydroxy C1-6 alkyl group, R4 represents a phenyl group which may be substituted with a carboxyl group, and m represents an integer of 1 to 3, with the proviso that a case where R1 is —CH2OH, and R3 is a C1-6 alkyl group, a C2-6 alkenyl group, or a benzyl group is excluded].

Abstract: Compounds are described that are useful for treating an apoptosis-associated disease, which are specifically cytotoxic to tumor cells that are overexpressing Bcl-xL, and are much less cytotoxic in isogenic cells that are not overexpressing Bcl-xL. Also described is a method for treating an apoptosis-associated disease in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of an active compound that is specifically cytotoxic to tumor cells that are overexpressing Bcl-xL, and are much less cytotoxic in isogenic cells that are not overexpressing Bcl-xL. Several scaffolds of active compounds are described.

Abstract: A reversely thermo-reversible hydrogel composition comprising a water soluble block copolymer comprising at least two blocks of polyethylene oxide and at least one block of polypropylene oxide, and at least one associative gelling adjuvant having water solubility less than 0.5 g/100 ml, preferably less than 0.3 g/100 ml at 20° C., and being capable of forming water soluble inter-molecular complexes with the water soluble block copolymer in water. The hydrogel composition exhibits improved gelling efficiency, enhanced solubility and/or stability for water sparely soluble and insoluble pharmaceutical agents. The hydrogel compositions are useful in a variety of pharmaceutical and cosmetic products and applications, such as esophageal, otic, vaginal, rectal, ophthalmic, treatments of disorders and imperfections of the skin, and treating and/or preventing alopecia and restoring and/or promoting hair growth.

Abstract: This invention provides a terbinafine pharmaceutical composition which is emulsifable or self-emulsifying or in form of an emulsion wherein the composition is adapted for oral administration.

Abstract: The invention relates to formulations of an antimicrobial agent, a lipid, and optionally a surfactant, and uses thereof for reducing the proliferation and viability of microbial agents.

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: Compositions and methods for the treatment and control of various conditions in an animal which comprises administering to said animal an effective amount of a immediate release composition of about 0.5% to 50% wt/wt of active ingredient together with excipients to a total of about 100%, wherein said compositon dissolves in a relatively short period of time, e.g., 75 seconds or less, 5 seconds or less, or 3 seconds or less, upon administration to said animal.

Abstract: This invention relates to bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable salts and their use in the modulation of Sirtuin 1 (Sirt1) and there use in neuroprotection for subject suffering from neurodegenerative diseases such as Alzheimer's disease, Huntington's disease, Amyotrophic lateral sclerosis, frontotemporal dementia, Parkinson's disease, including Parkinson's plus diseases such as multiple system atrophy, progressive supranuclear palsy, corticobasal degeneration and dementia with Lewy bodies, and in the manufacture of medicaments for such Sirt1 modulation and neuroprotection.

Abstract: The present invention discloses methods of use of facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers, including, but not limited to, pharmaceutical uses of the polymers and oligomers as antimicrobial agents and as antidotes for hemorrhagic complications associated with heparin therapy. The present invention also discloses novel facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers, compositions of the novel polymers and oligomers, including pharmaceutical compositions, and methods of designing and synthesizing the facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers.

Abstract: Compositions and methods are disclosed for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1). The compounds disclosed are amine-containing and amide-containing compounds. The compounds and compositions are useful for treatment of diseases, including inflammation, inflammatory diseases and autoimmune disorders.

Abstract: Novel polyamine transport inhibitors have been synthesized and demonstrated to block the uptake of native polyamines into human cancer cells. A combination therapy of the transport inhibitor and DFMO (a drug which blocks polyamine biosynthesis) provided synergistic activity against a metastatic human colon cancer cell line. The strategy uses polyamine depletion and polyamine metabolism to generate reactive oxygen species within cells as a novel way to treat cancers. This approach may be implemented for widespread use in the treatment of diseases which rely upon polyamine transport activity for proliferation.

Abstract: A method of treating and/or preventing oxidative damage, comprising administering an effective IsoK/NeuroK adduct formation suppressing amount of a phenolic amine compound and/or pyridoxamine or pyridoxamine analog, including embodiments where the phenolic compound is at least one of a pyridoxamine, salicylamine, tyrosine compound or an analog thereof.

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. In certain embodiments, the present invention comprises compositions comprising novel substituted ethylene diamine compounds further comprising antitubercular agents such as rifampicin, isoniazid, pyrazinamide and ethambutol.

Abstract: Memantine compositions and methods of use are described herein. In some embodiments, the compositions comprise memantine and an absorption enhancer, or memantine and an elimination enhancer, or memantine and an absorption enhancer and an elimination enhancer.

Abstract: Novel topical compositions for the treatment of nail and skin afflictions comprising at least one active agent, at least one volatile solvent, at least one film-forming ingredient and at least one phospholipid, processes for their preparation and methods of treatment of nail and skin afflictions. Following application of the compositions and evaporation of volatile solvents, the composition produces a film, which has web-like structures containing the active agent(s).

Abstract: The invention relates to methods for detecting the oncogenic condition of cells, including step where the amount of the OCDO compound in said cells is measured, and to the uses thereof. The invention further relates to OCDO inhibitors for use in methods for treating cancer.

Abstract: The invention provides a method for improving hair biology, e.g., hair growth. The method comprises administering to a subject a monoamine oxidase inhibitor and a vasodilator, a zinc salt of a carboxylic acid, a xanthine compound, pyrithione or a salt thereof, saponin, tritapene, crataegolic acid, celastrol, asiatic acid, an inhibitor of 5-alpha-reductase, 1,4-methyl-4-azasteroid, an androgen receptor antagonist, azelaic acid or a derivate thereof, cyclosporin, triiodothyronine, diazoxide, retinoic acid, a prostaglandin analogue, aminexil, carnitine tartrate, apigenin, procapil, or adenosine, in an amount effective to achieve a desired effect. The invention further provides a method of reducing or delaying the appearance of an age-related skin imperfection. The method comprises administering to the subject a composition comprising an MAO inhibitor. A kit for improving hair growth also is provided.

Abstract: The present invention provides compositions comprising allylamine drug compounds for topical treatment of fungal infections of the skin and skin appendages. In some embodiments a positive charge and enhancers are used in the compositions to allow for increased penetration of the active ingredient through skin and skin appendages. In some embodiments the positively charged active ingredients are either dissolved in the vehicle directly or dissolved in a plurality of beads suspended in the vehicle. The present invention also provides methods for making compositions comprising an allylamine drug compound, and methods of using such compositions for the treatment of fungal infections of the skin and skin appendages.

Abstract: The present invention relates to methods for reducing testosterone levels by reduction of luteinizing hormone (LH) or independent of LH levels in a male subject and methods of treating, suppressing, reducing the incidence, reducing the severity, or inhibiting prostate cancer, advanced prostate cancer, and castration-resistant prostate cancer (CRPC) and palliative treatment of prostate cancer, advanced prostate cancer and castration-resistant prostate cancer (CRPC). The compounds of this invention suppress free or total testosterone levels to castrate levels which may be used to treat prostate cancer, advanced prostate cancer, and CRPC without causing bone loss, decreased bone mineral density, increased risk of bone fractures, increased body fat, hot flashes and/or gynecomastia.

Abstract: Medicated single use, bilateral and bi-textured substrate uniformly impregnated with medicated anhydrous OTC (over-the-counter) solution for the topical use of aseptically delivering a single dose of medication to the surface of the skin. Medicate solution and substrate is contained encapsulated within a heat sealed foil enclosure that is stable for at least five years.

Abstract: Skin care compositions comprising certain substituted diamines, which are particularly beneficial for skin lightening and achieving evenness of color, especially for face and underarm skin.

Abstract: Compounds and their syntheses are disclosed herein. Compositions and pharmaceutical compositions comprising a compound are also described, and include compositions also comprising liposomes. Methods for the treatment of cancer in animals comprising administering a compound or a composition comprising a compound are also described.

Abstract: The invention relates to a pharmaceutical composition with a content in active ingredient that can be an antimycotic, so that the composition is suitable for the treatment of onychomycoses, in particular severe onychomycoses. The inventive formulation is an ointment-like thermogel at body temperature and an inviscid thermogel at lower temperatures and facilitates the permeation of sufficient active ingredient quantities through human fingernails and toenails, in order to also treat severe onychomycoses.

Abstract: The invention relates to an intermediate, obtainable by jointly compacting (i) crystalline cinacalcet or a pharmaceutically acceptable salt thereof, with (ii) a hydrophilising agent, and also tablets containing the intermediates of the invention. The invention further relates to cinacalcet tablets with a bimodal pore size distribution and a method of preparing the tablets of the invention. Finally, the invention relates to the use of a pH adjuster for preparing cinacalcet formulations which can preferably be administered independently of mealtimes.

Abstract: Provided herein are impurities of cinacalcet, (R)-?-methyl-N-[3-[3-(trifluoromethyl)phenyl]propyl]-1-(5,6,7,8-tetrahydronaphthalene)methaneamine (tetrahydro cinacalcet impurity), (R)-?-Methyl-N-[3-[3-(trifluoromethyl)phenyl]propyl]-1-naphthalenemethaneamine-N-oxide (cinacalcet N-oxide impurity) and (R)-?-methyl-N-[3-[3-(trifluoromethyl)phenyl]methyl]-1-naphthalenemethaneamine (benzylamine impurity); and processes for preparation and isolation thereof. Provided further herein is a highly pure cinacalcet or a pharmaceutically acceptable salt thereof substantially free of impurities, processes for the preparation thereof, and pharmaceutical compositions comprising highly pure cinacalcet or a pharmaceutically acceptable salt thereof substantially free of impurities.

Abstract: Polymeric anti-microbial agents produced by substituting the nitrogen atoms in the backbone of ethylenimine polymers, for example, substitution with aralkyl groups, are provided. The agents are believed to have low human toxicity while being effective against a variety of pathogens and are useful in applications involving human contact, such as cosmetics, hair care products and textiles, as well as in applications with much less human contact, such as coatings.

Abstract: The disclosure relates to novel compounds that are capable of modulating Jak2 kinase activities, compounds that have therapeutic use in treating or preventing a subject suffering from or susceptible to a Jak2 mediated disease or disorder, and methods of use and compositions thereof.

Abstract: The invention is directed to compositions comprising stable nanoparticulate cinacalcet or a salt thereof. The composition can exhibit an improved dissolution rate, improved bioavailability, and reduced difference in absorption when administered orally under fed as compared to fasting conditions. The invention also encompasses methods of making and using such compositions.

Abstract: Methods for treating and preventing otitis externa with a course of treatment consisting of as little as a single dose are provided. The methods are practiced by topical administration of compositions having a lipid carrier, such as liposomes and non-vesicular lipids, to the outer ear canal. Such compositions lack viscocity-enhancing celluloses or adhesives, and are preferably not in the form of a gel. Active agents useful for treating pain, inflammation, fungal or parasitic infestation and/or infections in the outer ear are co-administered in or with the composition.

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: The present invention relates to biocompatible oligomer-polymer compositions for the in situ formation of implants, wherein the implants release a bioactive agent, a metabolite, or a prodrug thereof, at a controlled rate. The sustained release delivery system includes a flowable composition containing a bioactive agent, a metabolite, or a prodrug thereof, and an implant containing a bioactive agent, a metabolite, or a prodrug thereof. The flowable composition may be injected into tissue whereupon it coagulates to become the solid or gel, monolithic implant. The flowable composition includes a biodegradable, thermoplastic polymer, a biocompatible end-capped oligomeric liquid, and a bioactive agent, a metabolite, or a prodrug thereof.

Abstract: A tissue adhesive including cyanoacrylate and polyethylene glycol (PEG), wherein the PEG remains a polyether and wherein the tissue adhesive is bioabsorbable. A tissue adhesive including cyanoacrylate bulk monomer and cyanoacrylate nanoparticles containing a therapeutic therein. A kit for applying a tissue adhesive, including the tissue adhesive described above and an applicator. Methods of accelerating degradation of a cyanoacrylate tissue adhesive applying a tissue adhesive, closing an internal wound, administering a therapeutic to tissue, treating cancer, and preventing infection in a wound. Methods of method of making a bioabsorbable tissue adhesive and making a therapeutic tissue adhesive.

Abstract: The invention provides a method for identifying a compound which modulates the activity of a BCL-2 family polypeptide, the method comprising: a) contacting said BCL-2 family polypeptide with a compound under conditions suitable for modulation of the activity of said BCL-2 family polypeptide; and b) detecting modulation of the activity of said BCL-2 family polypeptide by the compound, wherein the compound interacts with a binding site comprising one or more of an ?1 helix, ?2 helix, a loop between ?1-?2, ?.6 helix, and select residues of ?4, ?.5, and ?.8 helices in said BCL-2 family polypeptide; wherein the interaction of the compound with the binding site occurs at a horizontal hydrophobic groove with or without a perimeter of charged and hydrophilic residues, a superior juxta-loop, an inferior juxta-loop, or combination thereof.

Abstract: Described herein are methods, compositions and kits related to manipulating hematopoietic stem cells (HSC) and more particularly to methods, compositions and kits related to increasing the number of hematopoietic stem cells in vitro, ex vivo and/or in vivo. Also described are methods, compositions and kits related to making an expanded population of HSC and methods, compositions and kits related to using the expanded population of HSC. For example, HSC growth may be enhanced by contacting the nascent stem cells or HSC with an agent that stimulates the nitric oxide signaling pathway.

Abstract: A class of compounds useful in pharmaceutical compositions and methods for treating or preventing cancer is described. The compounds' ability to inhibit RET kinase is quantified, i.e., their respective RET IC50 and EC50 values are described. One such compound, known as cyclobenzaprine and herein as SW-01, has been identified as RET-specific with an IC50 of 300 nM. SW-01 inhibits RET autophosphorylation and blocks the growth and transformation of thyroid cancer cell lines. It has been further tested in pancreatic cancer, breast cancer, and SCLC cell lines. The compounds show utility for inhibition of survival and proliferation of tumour cells.

Abstract: The invention provides a pharmaceutical composition that can be used for efficient administration of low-molecular weight drugs and polymeric compounds such as peptides and proteins by methods other than injection, as well as a method for producing the composition. The pharmaceutical composition is for transmucosal administration and comprises (a) a drug having a positive or negative charge at a predetermined pH, (b) a pharmaceutically acceptable small particle and (c) a pharmaceutically acceptable surface-coating polymer capable of being electrically charged at the pH, wherein the surface of the small particle is coated by the surface-coating polymer, the drug is immobilized on the surface of the small particle via the surface-coating polymer, and a complex is formed by a noncovalent interaction between the small particle and the surface-coating polymer and a concurrent electrostatic interaction between the surface-coating polymer and the drug.

Abstract: The invention relates to a process for tightly controlling the particle size of cinacalcet hydrochloride, i.e. a process for preparing large or small crystals of cinacalcet hydrochloride, which yields cinacalcet hydrochloride in a narrow, reproducible and consistent distribution of particles, which hence does not require to reprocess, rework or destroy material of undesired size, which is efficient and cost-effective, and which is suitable for industrial implementation.

Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A? amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.

Abstract: Compositions intended for the percutaneous administration of physiologically active agents, e.g. drugs or a veterinary agents, are disclosed. Sasd compositions are characterized by having an exeefenf long term efficacy due to their ability to form a long-lasting film on the skin.

Abstract: The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators.

Abstract: An embodiment of the invention provides preventing or treating a viral infection of a host, comprising administering to the host an effective amount of an inhibitor of the protein LSD1 and/or a monoamine oxidase inhibitor. Another embodiment of the invention provides preventing or treating reactivation of a virus after latency in a host, comprising administering to the host an effective amount of an inhibitor of the protein LSD1 and/or a monoamine oxidase inhibitor. Another embodiment of the invention provides preventing or treating a viral infection in a mammal that has undergone, is undergoing, or will undergo an organ or tissue transplant, comprising administering to the mammal an effective amount of an inhibitor of the protein LSD1 and/or a monoamine oxidase inhibitor before, during, and/or after the organ or tissue transplant. The viral infection may be due to a herpesvirus, such as herpes simplex virus type 1 (HSV-1) or type 2 (HSV-2), varicella zoster virus (VZV), or cytomegalovirus (CMV).