Abstract: Stilbene analogs and pharmaceutical compositions that are useful for the treatment of various cancers, including without limitation, colorectal cancer (CRC) and breast cancer are disclosed. The halogenated stilbene analogs include nitrogen heteroaryl groups and/or amino groups on the stilbene ring.

Abstract: A method is provided for the treatment of vision problems in a subject suffering from one of various forms of albinism, including, for example, oculocutaneous albinism types OCA1a and OCA1b, as well as ocular albinism type 1, resulting from mutations in the GPR143 gene, as well as the OCA2, OCA3 or OCA4 genes, by administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of the compound (2-[2-nitro-4-(trifluoromethyl)benzoyl]cyclohexane-1,3-dione), also known as NTBC for a sufficient period of time. The administration of NTBC is believed to increase the amount of pigmentation in the subject and alleviate certain symptoms caused by lack of pigmentation in the eye tissues. Also described are methods of use of NTBC for increasing the pigmentation of a subject for cosmetic purposes, by administering to the subject a therapeutically effective amount of NTBC.

Abstract: The present invention relates to extended release dosage forms of metoprolol or salts thereof comprising a water insoluble and non-swellable inert core and one or more pharmaceutically acceptable excipients. The invention also relates to processes for the preparation of an inert core and extended release dosage forms.

Abstract: The present invention provides N-alkylthio ?-lactams and disulfide compounds (e.g., alkyl-coenzyme A asymmetric disulfides or aryl-alkyl disulfides), compositions containing such compounds, and methods of their use as anti-bacterial agents.

Abstract: A method of treating an ocular disorder in a subject associated with aberrant all-trans-retinal clearance in the retina, the method comprising administering to the subject a therapeutically effective amount of a primary amine compound of formula: wherein R1 is an aliphatic and/or aromatic compound.

Abstract: Therapeutic compositions and methods for treatment of late-onset Gaucher disease are described herein. The compositions comprise compounds having activity as pharmacological chaperones for mutant forms of the beta-glucocerebrosidase. Methods of treatment involve providing therapeutically effective amounts of such compositions to subjects in need thereof.

Abstract: The present invention relates to a novel compound having excellent antioxidant activity, isolated from Ramalina terebrata, and more particularly to a novel compound, RAMALIN™, having excellent antioxidant activity, isolated from the Antarctic lichen Ramalina terebrata, a method for preparing the RAMALIN™, and a pharmaceutical composition, a functional food and a functional cosmetic composition, which contain the RAMALIN™ as an active ingredient. The RAMALIN™ according to the invention has significantly excellent antioxidant effects compared to commercially available antioxidants, and thus can be widely used in agents for treating oxidation-related diseases, anti-aging functional foods, functional cosmetic products for skin whitening and wrinkle reduction, etc.

Abstract: Provided are compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.

Abstract: Provided are analgesic compounds, and salts thereof, of formula: (I) wherein A is: (A) Additionally, pharmaceutical formulations and methods of use employing the above compounds are provided.

Abstract: The invention relates to hydroxyphenyl derivatives of formula (I); and uses thereof as anti-bacterial and/or anti-parasitic agents.

Abstract: The invention provides starch-based microparticles with high loading capacity for the stabilization and/or controlled release of one or more agents, for example, a pharmaceutical, a taste masking agent, a flavoring agent, or a combination thereof, disposed within the microparticles, and to methods of making and using such microparticles.

Abstract: The invention relates to compounds that modulate the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds are act as modulators or potentiators of GLP-1 receptor on their own, or with receptor ligands including GLP-1 peptides GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.

Abstract: The invention relates to phosphorylation inhibitor compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating cell proliferative disorders, especially cancer.

Abstract: Disclosed is a misuse preventative, controlled release formulation comprising a core comprising a superabsorbent material (for example, polycarbophil), a controlled release coat surrounding the core, and a plurality of controlled release microparticles having a pharmaceutically active agent (for example, an opioid analgesic) disposed within the core, the coat, or both the core and the coat. When crushed, either intentionally or accidentally, and exposed to an aqueous medium, the superabsorbent material present in the coreswells to encapsulate the microparticles, which remain substantially intact thereby retarding the release of the pharmaceutically active agent from the formulation. Also disclosed is a method of using the misuse preventative, controlled release formulation to deliver a pharmaceutically active agent to a mammal, for example, a human, in need thereof.

Abstract: The present invention relates to a pharmaceutical composition of practically water insoluble or low water soluble compounds containing catechol moiety by enhancing the solubility of such compounds using one or more alkalizing agent and optionally adding one or more pharmaceutically acceptable excipient. The present invention also relates to a process for preparing such pharmaceutical composition.

Abstract: Cannabionid receptor-2 inverse antagonists include compounds represented by Formula IV, or a pharmaceutically acceptable salt thereof: wherein: R1 and R2 are independently H, alkyl, or alkenyl; R3 is alkyl, alkenyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl; R4 and R5 are independently a bond, alkylenyl, or alkenylenyl; each R6 and R7 is independently selected from the group consisting of OH, F, Cl, Br, I, (C1-C6)alkyl, alkoxy, amino, COOH, CONH2, SO3H, PO3H2, CN, SH, NO2 and CF3; and p and q are independently 0, 1, 2, 3, 4, or 5. Such compounds may be used to treat osteoporosis or multiple myeloma.

Abstract: A method of forming an ocular delivery device includes exposing a solid, shaped cellulose polymer to a solution including an active pharmaceutical ingredient (API) and a solvent capable of solubilizing the API, wherein the polymer absorbs at least a portion of the solution, including the API and solvent. The method may further include removing at least a portion of the absorbed solvent from the polymer by allowing the absorbed solvent to evaporate from the polymer or by drying the polymer. A variety of cellulose polymers may be used, including hydroxypropyl cellulose. A variety of APIs may be used, including Cyclosporine, Tobramycin and Vancomycin. Ocular delivery devices prepared by the methods may be used to treat a variety of eye disorders.

Abstract: The present invention relates to the use of a nitroaniline derivative of Formula I for the production of nitric oxide and for the preparation of a medicament for the treatment of a disease wherein the administration of nitric oxide is beneficial. The present invention furthermore relates to a method for the production of NO irradiating a nitroaniline derivative of Formula I, a kit comprising a nitroaniline derivative of Formula I and a carrier and to a system comprising a source of radiations and a container associated to a nitroaniline derivative of Formula I. In Formula I, R and RI are each independently hydrogen or a C1-C3 alkyl group; RII is hydrogen or an alkyl group.

Abstract: Disclosed is a concentrate for dilution comprising a S1P receptor agonist or a pharmaceutically acceptable salt thereof, propylene glycol and optionally glycerin. This formulation is adapted for patients in a difficult condition to swallow.

Abstract: The present invention is directed to pharmaceutical compositions of effective amounts of NMDA receptor antagonists and preservative for the administration to a patient in need of effective analgesia and anesthesia. The compositions of the invention advantageously do not cause any significant neurotoxicity. The preferred NMDA receptor antagonist is ketamine. The preferred preservative is benzalkonium chloride.

Abstract: The invention relates to a dosage form that is thermoformed without discoloration and is safeguarded from abuse, comprising at least one synthetic or natural polymer having a breaking strength of at least 500 N in addition to one or more active substances that could be subject to abuse. The invention also relates to a corresponding method for producing said dosage form.

Abstract: The present invention relates to an If blocker or a pharmaceutically acceptable salt thereof for the treatment and/or prevention of a canine patient suffering from heart diseases, preferably heart diseases such as dilated cardiomyopathy (DCM), mitral valve insufficiency (MI), arrthymias, preferably tachyarrthymias, preferably arterial arrhythmias, atrioventricular nodal arrhythmias and/or tachycardia. Each of these diseases may or may not result in heart failure (HF) in canine patients. The invention also relates to improving the quality of life, improving the general health condition as well as a prolonging the life expectancy in canine patients suffering from heart diseases and/or heart failure due to one or more of the following etiologies dilated cardiomyopathy (DCM), mitral valve insufficiency (MI), arrthymias, preferably tachyarrthymias, preferably arterial arrhythmias, atrioventricular nodal arrhythmias and/or tachycardia.

Abstract: The present invention relates to a process for the production of an abuse-proofed solid dosage form containing at least one active ingredient with potential for abuse and a binder with a breaking strength of ?500 N, by exposing a mixture comprising the active ingredient and the binder to ultrasound and force.

Abstract: An agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that activates a serotonin 5-HT2C receptor, an agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that stimulates an androgen binding site, and a method of screening for a drug for the prophylaxis or treatment of abdominal pressure incontinence, which includes electrostimulating the abdominal muscles or a nerve controlling them of an animal to increase the abdominal pressure, and measuring the leak point pressure at that time.

Abstract: Use of Pargyline for the production of a medicament for influencing the metabolism of hair follicles and the modulation of their vital cycle.

Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein Y, L, A, W1, W2, and R?1 are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.

Abstract: The present invention relates to the use of compounds of the invention for treatment and/or prevention of fatigue, including fatigue associated with diseases or treatments.

Abstract: The present invention relates to stable pharmaceutical compositions comprising entacapone, levodopa and carbidopa, or pharmaceutically acceptable salts or hydrates thereof. The invention also relates to processes for the preparation of such compositions.

Abstract: Dapsone and dapsone/adapalene compositions can be useful for treating a variety of dermatological conditions. The compositions of this disclosure include dapsone and/or adapalene in a polymeric viscosity builder. Subject compositions can be adjusted to optimize the dermal delivery profile of dapsone to effectively treat dermatological conditions and improve the efficiency of pharmaceutical products applied to the skin. Use of the polymeric viscosity builder provides compositions with increased concentrations of diethylene glycol monoethyl ether relative to compositions without the polymeric viscosity builder.

Abstract: The present disclosure provides functionalized magnetic nanoparticles (MNPs) comprising a functional group that binds to ?-amyloid deposits and/or neurofibrillary tangles. The present disclosure provides compositions comprising the functionalized MNPs, and methods of using the functionalized MNPs in imaging ?-amyloid deposits and neurofibrillary tangles.

Abstract: A method of treating an ocular disorder in a subject associated with aberrant all-trans-retinal clearance in the retina, the method comprising administering to the subject a therapeutically effective amount of a primary amine compound of formula: wherein R1 is an aliphatic and/or aromatic compound.

Abstract: Tramadol or a pharmaceutically acceptable salt thereof is used in the manufacture of a pharmaceutical preparation for the treatment of functional gastrointestinal disorders such as irritable bowel syndrome.

Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein A, Y, L, R1, W1 and W2 are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.

Abstract: Phenyl-substituted cyclohexylamine derivatives and method for their synthesis and characterization are disclosed. Use of these compounds to treat/prevent neurological disorders as well as methods for their synthesis are set forth herein. Exemplary compounds of the invention inhibit reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine (e.g., from the synaptic cleft) and modulate one or more monoamine transporter. Pharmaceutical formulations incorporating compounds of the invention are also provided.

Abstract: Clenbuterol or its salt for use in the treatment of autism, in particular pediatric autism. Improved contact with surroundings, better concentration, improved ability to plan a specific task, improved understanding, calming, and reduced psychomotor anxiety were observed.

Abstract: The present invention relates to an abuse-proofed, thermoformed dosage form containing, in addition to one or more active ingredients with abuse potential optionally together with physiologically acceptable auxiliary substances, at least one synthetic or natural polymer with a breaking strength of at least 500 N and to a process for the production thereof.

Abstract: The present invention is directed to methods for the treatment of treatment-refractory depression or treatment-resistant depression comprising administering to a patient in need thereof, a therapeutically effective amount of esketamine as mono-therapy or as combination therapy with at least on antidepressant.

Abstract: The invention relates to a dosage form that is thermoshaped without being extruded and that is safeguarded from abuse, comprising at least one synthetic or natural polymer having a breaking strength of at least 500 N in addition to one or more active substances that could be subject to abuse and optionally physiologically acceptable adjuvants. The invention also relates to a corresponding method for producing said dosage form.

Abstract: Aqueous compositions suitable for topical administration to the human or animal eye contain at least one water-soluble polymeric ophthalmic lubricant, such as hyaluronate, carbomer gel or hypromellose, together with a water-soluble analgesic. The analgesic may be an opiod, particularly an opioid having an affinity for 5-HT receptors, such as tramadol. Typical tramadol levels would be in the range of 0.5% to 1.0% w/v. The aqueous compositions may for example be used as artificial tears, and as general ophthalmic lubricants for treating conditions such as dry eye or blepharitis. Further compositions combine ophthalmologically-active agents, such as pharmaceuticals, with opioids, such as tramadol in particular. These compositions may be used to treat the eye while reducing pain or discomfort that would normally be produced by administering these particular pharmaceuticals to the eye, and increasing the efficacy of the pharmaceuticals.

Abstract: The present invention aims to demonstrate that a soluble pharmaceutical formulation can be prepared of N,N?-Diamino-diphenyl sulfone which is useful in the development of an ideal drug for use against cerebral infarction, epilepsy, traumatic spinal cord injury, cranio-encephalic trauma, leprosy, Pneumocystis carinii infections and any condition which requires rapid and complete absorption of the compound. As a representative example of this application, the dissolution of N,N?-Diamino-diphenyl sulfone was evaluated as a neuroprotector in a model of acute cerebral infarction in rats. In this study, N,N?-Diamino-diphenyl sulfone showed significant prevention of brain damage, without presenting adverse effects in animals. It is also shown that the soluble pharmaceutical formulations prepared in this manner produce peak blood levels 30 minutes from oral administration and immediately via the intravenous route.

Abstract: The invention relates to a dosage form comprising a physiologically effective amount of a physiologically active substance (A), a synthetic, semi-synthetic or natural polymer (C), optionally one or more physiologically acceptable auxiliary substances (B) and optionally a synthetic, semi-synthetic or natural wax (D), wherein the dosage form exhibits a resistance to crushing of at least 400 N and wherein under physiological conditions the release of the physiologically active substance (A) from the dosage form is at least partially delayed.

Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.

Abstract: A scleral lens is provided with a sodium channel blocker or a sodium channel modulator disposed in the pre-corneal tear film between the scleral lens and the cornea. This system can be used to deliver sodium channel blockers or a sodium channel modulators not currently used because of poor bioavailability. Methods of using this sodium channel blocker delivery system or a sodium channel modulator delivery system are also disclosed.

Abstract: Embodiments of the present invention are directed to compositions and methods for the treatment of purpura. Preferred compositions comprise an ? adrenergic receptor agonist selected from selective ?1 adrenergic receptor agonist, selective ?2 adrenergic receptor agonist, non-selective ?1/?2 adrenergic receptor agonist, agents with ?2 adrenergic receptor agonist activity and combinations thereof, in a pharmaceutically acceptable carrier in order to treat and improve the cosmetic appearance of hemorrhagic (purpuric) lesions in the skin.

Abstract: Disclosed is an external preparation composition having good transdermal absorbability. An external preparation composition having excellent transdermal absorbability can be produced by dissolving a medicinal substance or a salt thereof in a fatty acid-based ionic liquid to form a composite ionic composition of the medicinal substance. The external preparation composition can be used as a liquid preparation, an ointment, a cream, a plaster or the like, and enables to provide a preparation having excellent transdermal absorbability.

Abstract: A multilayer oral dosage form that provides controlled release of an active compound includes a non-erodible core containing a pharmaceutically active compound and/or a nutritionally active compound, and at least one release-modulating layer laminated to each side of the core layer. The dosage form can be prepared using simple, inexpensive tablet compression techniques.

Abstract: A wood treatment composition having a synergistic combination of fungicides which may include two or more compounds. These combinations are shown to be especially effective in providing resistance to decay, mold and mildew when wood is treated with these combinations. Also provided is wood treated by these combinations, and a method of treatment for composite wood.

Abstract: External preparations for athlete's foot treatment capable of enhancing patient's compliance and capable of reducing the symptom of rubefaction, comprising an anti-trichophyton drug mixed with at least one compound selected from among 1-menthol, menthol analogue compounds and bactericidal compounds.

Abstract: The present invention provides a method of selectively inhibiting PKC? in the presence of PKC?, by administering to a subject in need thereof, a therapeutically effective amount of a compound of Formula I. The present invention also provides a method of inhibiting cytokine synthesis in a T cell, a method of inhibiting T cell proliferation, and a method of inhibiting the replication of and cytokine production by T lymphocytes, while not stimulating or inhibiting the replication of B lymphocytes.

Abstract: Stilbene analogs and pharmaceutical compositions that are useful for the treatment of various cancers, including without limitation, colorectal cancer (CRC) and breast cancer are disclosed. Such stilbene analogs include, for example, compounds of the following formula: wherein Ra, Rb, R4, R6, R7, R9 and R10 are all H; R2 and R3 are independently H, halo, amino, alkylamino, dialkylamino, N-oxides of dialkylamino, arylalkylamino, trialkylammonium, mercapto, alkylthio, alkanoyl, nitro, nitrosyl, cyano, alkoxy, alkenyloxy, aryl, heteroaryl, sulfonyl, sulfonamide, CONR11R12, NR11CO(R13), NR11COO(R13) or NR11CONR12R13; R11, R12 and R13, are independently, H, alkyl, aryl, heteroaryl or a fluorine; R8 is NRCRdZ wherein Rc is H, alkyl, alkoxy, aryl or heteroaryl, Rd is an alkyl group, Z is a an unshared pair of electrons, H, alkyl or oxygen; and R1 and R5 are halogen.