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: Provided are compounds which generally have a triketone structure. Examples of the compounds include derivatives of 1,3-cyclohexanedione, such as: 1,3-cyclohexanedione, 2-propanoyl-5-cyclohexyl-; 1,3-cyclohexanedione, 2-propanoyl-5-[4-fluorophenyl]-; 1,3-cyclohexanedione, 2-acetyl-5-[thien-2-yl]-; 1,3-cyclohexanedione, 2-acetyl-5-butyl-; and 1,3-cyclohexanedione, 2-propanoyl-5-[bicyclo[2.2.1]hept-2-en-5-yl]-. The compounds can be used to alter the lifespan of eukaryotic organisms and treat inflammation.

Abstract: The present invention relates to a compound of Formula 1, wherein: (A) is heteroaryl or aryl; each (A?), if present, is independently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A?) is substituted with 0, 1, 2, or 3 substituents independently chosen from halo, haloalkyl, haloalkoxy, aryl, arylalkoxy, alkyl, alkoxy, amido, —CH2C(=0)NH2, heteroaryl, cyano, sulfonyl, and sulfinyl; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is —NH—; (L) is chosen from a single bond, —CH2—, —CH2CH2—, —CH2CH2CH2—, and —CH2CH2CH2CH2—; and (D) is an aliphatic carbocyclic group or benzocycloalkyl, wherein said aliphatic carbocyclic group or said benzocycloalkyl has 0, 1, 2, or 3 substituents independently chosen from —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), alkyl, halo, amido, cyano, alkoxy, haloalkyl, and haloalkoxy.

Abstract: The present embodiments relate to topically delivered medication (compounded) for treatment of pain, inflammation, muscle fatigue, spasms, and/or other ailments. A transdermal cream may provide the effective topical administration of multiple medications simultaneously. The transdermal cream may include a salt load of approximately 30% or greater. The transdermal cream may include a unique base composition such that the transdermal cream may be able to remain stable and avoid degradation for six months or more and capable of effective delivery of active ingredient concentrations exceeding approximately 40% or more of the total formulation weight. The active ingredients may include a nerve depressant, NSAID, muscle relaxant, opiate agonist, local anesthetic, NMDA receptor antagonist, and a tricyclic antidepressant. In one embodiment, the transdermal cream may comprise ketamine HCL, gabapentin, clonidine HCL and baclofen.

Abstract: The present invention provides a compound represented by the following formula (I); [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like; formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a phenylene group and the like which may condense with a 5- to 6-membered ring and may have a heteroatom; Ra and Rb are the same as or different from each other and represent a hydrogen atom and the like; W represents a single bond and the like; R? represents 1 to 4 independent hydrogen atoms and the like; and R? represents 1 to 4 independent hydrogen atoms and the like] or a salt thereof, or a hydrate thereof.

Abstract: This disclosure describes methods of screening for compounds that disrupt the interaction between DNMT1 and the gamma-globin promoter or between LSD-1 and the gamma-globin promoter. This disclosure describes methods of screening for compounds that de-repress the gamma-globin gene.

Abstract: Described herein are arylcyclopropylamine compounds that may inhibit enzymes comprising an amine oxidase domain, such as LSD1, MAO A and/or MAO B.

Abstract: Treatment of CNS disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is also disclosed. The process includes the preparation of all four isomers of N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-yl]formamide, which are also useful.

Abstract: Administration of a monoamine oxidase inhibitor is useful in the prevention and treatment of muscle dystrophy. Methods and compositions for inhibiting the production of reactive oxygen species in a muscle cell overproducing reactive oxygen species are provided herein.

Abstract: The invention describes essentially a non-therapeutical process for deterring vermin, which is based on the usage of the largely known beta amino-alcohol derivatives of formula (I), as defined herein before. Furthermore, it describes the corresponding vermin-deterring compositions which contain these substances as the active ingredient, compounds of the formula (I) for the preparation of vermin-deterring compositions, and the use of compounds of formula (I) in the defense against vermin. Thus, the invention describes how and in which form the compounds of the formula (I) or their acid addition salts are used to deter vermin from materials, places or warm-blooded animals.

Abstract: The present invention provides sphingosine-1-phosphate analogs that are potent, and selective agonists at one or more S1P receptors, specifically the S1P1 receptor type, which alter lymphocyte trafficking. The compounds of the invention include compounds having a phosphate moiety as well as compounds with hydrolysis-resistant phosphate surrogates such as phosphonates, alpha-substituted phosphonates, and phosphothionates.

Abstract: The present invention is drawn to adhesive formulations and methods of drug delivery. The formulation can include a drug, a solvent vehicle, and a solidifying agent. The solvent vehicle can include a volatile solvent system including at least two volatile solvents, and a non-volatile solvent system including at least one non-volatile solvent, wherein at least one non-volatile solvent is capable of facilitating the delivery of the drug at therapeutically effective rates over a sustained period of time. The formulation can have a viscosity suitable for application to a skin surface prior to evaporation of the volatile solvents system. When applied to the skin, the formulation can form a solidified layer after at least a portion of the volatile solvent system is evaporated.

Abstract: Compositions for the topical or transdermal treatment of neuropathy. More particularly, transdermal or topical compositions including a combination of ingredients that provide a surprising degree of effective relief from the symptoms of peripheral neuropathy are described.

Abstract: The present invention relates to the identification of provided cyclohexane-1,3-diones (CHD compounds) and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the provided CHD compounds.

Abstract: The use of dapsone is the first effective treatment against the disabling consequences associated with cerebral infarction in patients. Dapsone was evaluated as a neuroprotector in the cerebral infarction model produced by the occlusion of the middle cerebral artery in rats and in patients suffering from acute cerebral infarction caused by thromboembolism. In both studies, dapsone displayed a reduction of between 70 and 90% in the adverse effects which occur as a consequence of the infarction.

Abstract: The present invention relates to compositions and methods that modulate at least one TRP family member. Specifically, the present invention relates to novel TRPA1 antagonists and their use in the treatment of pain such as chronic inflammatory and neuropathic pain. Compounds that can modulate one or more TRPA1 functions are useful in many aspects including, but not limited to, maintaining calcium homeostasis; maintaining sodium homeostasis; modulating intracellular calcium levels; modulating membrane polarization (membrane potential); modulating cation levels; and/or treating or preventing diseases, disorders, or conditions associated with calcium homeostasis, sodium homeostasis, calcium or sodium dyshomeostasis, or membrane polarization/hyperpolarization (including hypo and hyperexcitability), and/or treating or preventing diseases, disorders, or conditions associated with regulation or misregulation of TRPA1 expression or function.

Abstract: The present invention features compositions and methods for treating cancers such as melanoma, which have a subpopulation of self-renewing JARIDIB-positive cells essential to maintenance and metastatic progression of the cancer.

Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.

Abstract: The present invention relates to novel biomarker for breast cancer, namely LSD1 and its application in inter alia the diagnosis of breast cancer. Furthermore, the present invention discloses a method of determining the LSD1 protein amount and the effect of LSD1 inhibitors on cancer cells selected from breast cancer, lung carcinoma and sarcoma.

Abstract: The subject invention provides a method of treating or inhibiting hearing loss in a mammalian subject. The method includes administering to a mammalian subject an amount of R(+)-N-propargyl-1-aminoindan or pharmaceutically acceptable salt thereof effective to treat or inhibit the hearing loss in the subject.

Abstract: The invention relates to novel calcium-sensing receptor (CaSR) modulating trifluoromethylphenylene cyclopentylene compounds represented in formula (I) and derivatives thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.

Abstract: The invention relates to novel calcium-sensing receptor (CaSR) modulating substituted cyclopentylene compounds represented in formula I and derivatives thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.

Abstract: Disclosed is crystalline R(+)-N-propargyl-1-aminoindan containing water at an amount of less than 0.5% by weight and a pharmaceutical composition comprising the same, and the process for the manufacture and the validation thereof. Also disclosed is a process for the preparation of solid rasagiline base.

Abstract: A method and apparatus for delivering a plurality of medicaments in a single delivery vehicle for the management of co-morbid diseases, illnesses and conditions. The present invention provides a novel delivery process for many medicaments. Medicaments may be encapsulated and stored separately within a larger capsule until the time of ingestion, consumption, or the like. Benefits of the present invention include maintaining separation of distinct ingredients within a single capsule and the capability to control the time release of multiple ingredients within the capsule.

Abstract: Provided herein are methods of and compositions for, treating, preventing and managing various neurological disorders. The methods comprise administering a transnorsertraline in combination with a serotonin receptor IA agonist, antagonist or modulator.

Abstract: The invention relates to novel salts of the active substance rasagiline. The salts show excellent processability even after prolonged storage and an excellent storage stability usually superior to known salts after being processed into tablets.

Abstract: The present invention concerns compositions, methods and/or apparatus of central administration of various CNS-ac-Live agents. In particular embodiments, intrathecal administration is advantageous for decreasing the systemic concentrations of CNS agent, thereby decreasing side effect toxicity, while allowing more effective delivery of the agent to the site of action, simultaneously decreasing the dosage delivered to the subject. In particular embodiments, ICV delivery may be of use for patients who have previously proven to be refractory to systemic administration of CNS agents, in some cases due to systemic side effects, or for those patients whose symptoms are of sufficient severity to warrant more aggressive therapeutic intervention. ICV administration allows not only lower systemic concentration but also higher therapeutically effective concentration within the CNS.

Abstract: Treatment of CNS disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is also disclosed. The process includes the preparation of all four isomers of N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-yl]formamide, which are also useful.

Abstract: The present invention relates to a method of treating or alleviating the symptoms of amblyopia. It is based on the discovery that repeated administration of a specific drug, which is known to be clinically active to treat depression in humans, results in improved vision of the amblyopic eye.

Abstract: The present invention is a method for increasing serotonin activity in mammary glands such that involution of milk secretion of the same mammary glands occurs. The present invention further is a composition that can be implanted, or infused into the mammary glands to cause involution of milk secretion.

Abstract: The invention provides methods for detection of medical disorders, associated with cellular oxidative stress, cell degeneration and/or cell death. The invention further relates to compounds comprising a thiol (—SH) group, for detecting cells undergoing oxidative stress, degeneration and/or a death process. The invention further provides methods for utilizing the compounds in medical practice, for diagnostic and therapeutic purposes.

Abstract: The present invention relates to phenylcyclopropylamine derivatives. In particular, pharmaceutical compositions comprising phenylcyclopropylamine derivatives are provided. The compounds of this invention can, inter alia, be used for the treatment and the prevention of cancer as well as neurodegenerative diseases or disorders.

Abstract: The present invention provides a compound represented by the following formula (I); [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like; formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a phenylene group and the like which may condense with a 5- to 6-membered ring and may have a heteroatom; Ra and Rb are the same as or different from each other and represent a hydrogen atom and the like; W represents a single bond and the like; R? represents 1 to 4 independent hydrogen atoms and the like; and R? represents 1 to 4 independent hydrogen atoms and the like] or a salt thereof, or a hydrate thereof.

Abstract: Disclosed are formulations which are designed to delay release of rasagiline while maintaining specific pharmacokinetic properties.

Abstract: A pharmaceutical combination comprising as components (a) at least one 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol compound, and (b) at least one NMDA-antagonist, a pharmaceutical formulation and a dosage form comprising such a combination, and a method of treating pain, e.g. inflammatory pain or neuropathic pain, in which components (a) and (b) are administered simultaneously or sequentially to a mammal, with component (a) being administered either before or after component (b), and with components (a) or (b) being administered to the mammal either via the same pathway of administration or via different pathways of administration.

Abstract: The invention relates to novel tetralone based amines and their use in the treatment of central nervous system (CNS) disorders, such as depression, attention deficit hyperactivity disorder (ADHD) and Parkinson's disease. The invention further relates to pharmaceutical compositions containing the compounds and compositions of the invention as well as methods of inhibiting reuptake of one or more monoamine, such as such as dopamine and norepinephrine, from the synaptic cleft, and methods of modulating one or more monoamine transporter.

Abstract: A crystalline salt of 3-[2-(dimethylamino)methyl(cyclohex-1-yl)]phenol and hydrogen chloride, preferably in a 1:1 composition, including various crystalline forms of this salt, processes for preparing the various crystalline forms of this salt, pharmaceutical compositions containing the various crystalline forms of this salt, and the use of this salt as a pharmacologically active agent in a pharmaceutical composition to treat or inhibit pain or other disorders or disease states.

Abstract: The present invention provides methods for treating cancer and other pathological proliferating conditions by inhibiting mitosis using at least one pyrrolo[2,3-d]pyrimidine having the general formula (16): where X is selected from the group consisting of lower alkyls, heteroalkyls, substituted or unsubstituted aryls or heteroaryls, arylalkyls, and heteroarylalkyls; where R1 is selected from the group consisting of hydrogen, lower alkyls, heteroalkyls, substituted or unsubstituted aryls or heteroaryls, arylalkyls, and heteroarylalkyls; where R2 is selected from the group consisting of hydrogen, lower alkyls, heteroalkyls, alkoxys, substituted or unsubstituted aryls or heteroaryls; where R3 is selected from the group consisting of zero, lower alkyls, heteroalkyls, alkenyls, and heteroalkenyls; and where R4 is selected from the group consisting of substituted or unsubstituted aryls or heteroaryls, arylalkyls, heteroarylalkyls, and hydrogen.

Abstract: Compounds and methods useful for preventing and treating pain, e.g., neuropathic pain, in a subject in need thereof are provided. The compounds can be “S1P modulating” agents that are capable of inducing a detectable change in S1P receptor activity.

Abstract: A controlled release dosage form has a coated core with the core comprising a drug-containing composition and a water-swellable composition, each occupying separate regions within the core. The drug-containing composition comprises a low-solubility drug and a drug-entraining agent. The coating around the core is water-permeable, water-insoluble and has at least one delivery port therethrough. A variety of formulations having specific drug release profiles are disclosed.

Abstract: Topical treatments for neuropathy are described. The treatments include topical formulations of NMDA antagonists and one additional active ingredient. In one example, the formulation includes ketamine and gabapentin for the treatment of a subject's neuropathy. These transdermal or topical compositions provide a surprising degree of effective relief from the symptoms of peripheral neuropathy and can be administered to subjects to treat various neuropathies.

Abstract: Disclosed is crystalline R(+)-N-propargyl-l-aminoindan containing water at an amount of less than 0.5% by weight and a pharmaceutical composition comprising the same, and the process for the manufacture and the validation thereof. Also disclosed is a process for the preparation of solid rasagiline base.

Abstract: Methods of attenuating the toxic or medically undesirable effects of drugs and toxins in a human by administering to a human an injectable formulation comprised of a dispersion of particles comprised of reversed cubic or reversed hexagonal lyotropic liquid crystalline material. The particles absorb or adsorb or otherwise sequester and attenuate the effect of drugs and toxins, and may be used as a rescue or reversal agent, or as a prophylaxis. The invention is especially applicable in reversing adverse effects of local anesthetics inadvertently delivered systemically, and attenuating the therapeutic effects of general anesthetics in the course of treatment.

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).

Abstract: This invention relates to combination therapies for the treatment of breast cancer comprising administering to a subject in need thereof a compound of Formula I or a pharmaceutically acceptable salt thereof and an anti-estrogenic agent (e.g., an aromatase inhibitor, a SERM that is not the SERM of Formula I, a GNRH agonist, a GNRH antagonist, or an estrogen receptor downregulator) and to compositions (e.g., pharmaceutical compositions) comprising a compound of Formula I or a pharmaceutically acceptable salt thereof and an anti-estrogenic agent. This invention also relates to a method of treating the side effects (e.g., vasomotor disturbances, osteoporosis and musculoskeletal complaints) associated with anti-estrogen therapy in a subject treated with one or more anti-estrogenic agents (e.g., an aromatase inhibitor, a SERM that is not the SERM of Formula I, a GNRH agonist, a GNRH antagonist or an estrogen receptor downregulator).

Abstract: The disclosure provides compounds and methods of using Apogossypolone derivatives for treating diseases and disorders. In particular, the disclosure provides compounds of Formula I: or a pharmaceutically acceptable salt, hydrate, or solvate thereof, and provides methods for the preparation of compounds of Formula I; and methods for treating cancer, autoimmune diseases, and inflammation by administering a compound of Formula I.

Abstract: This invention relates to novel triaryl derivatives, formula (I), a stereoisomer thereof or a mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein all of X, Y and Z represent CH; or one or two of X, Y and Z represent N; and the others of X, Y and Z represent CH; and R1, R2, R3, R4 and R5. independently of each other, represent hydrogen, halo, tri-fluoromethyl, trifluoromethoxy, cyano, hydroxyl, alkoxy, alkyl, amino or sulfamoyl; or R1 and R2, together with the phenyl ring to which they are attached form an indolyl ring or a benzo-dioxolyl ring; and R3, R4 and R5 are as defined above; and R6 represents amino or nitro, which are found to be modulators of the nicotinic acetylcholine receptors.

Abstract: A method for the treatment and prophylaxis of conditions of aging due oxidative stress and as growth factors of stem cells. Such conditions due to oxidative stress are associated with a decreased presence of one or more cell-specific carbonic anhydrase enzymes in the tissue of a subject. Such conditions include but are not limited to alzheimer's disease, parkinson's disease, multiple sclerosis, autism, lou gehrig's disease, huntington's disease, diabetes mellitus, amyloid diseases, atherosclerosis, arthritis, osteoporosis, cystic fibrosis. The method comprises administering to the patient a pharmaceutically effective, non-toxic amount of one or more compounds that increases the presence of one or more Carbonic Anhydrase Isozymes whose levels have been reduced in the subject.

Abstract: This invention describes a topical delivery mechanism that contains a mixture of cetylated fatty esters that act as transdermal carriers of desired therapeutic molecules. The proposed cetyl fatty ester penetrant-complex (Base CFEP-complex) contains specific cetyl fatty esters, polar solvents, a carrier base (gel, cream, lotion, patch or stick gel), antioxidants and the desired pharmaceutical, cosmetic or antigenic response eliciting molecules that are efficaciously delivered by selectively varying component ratios in the complex.

Abstract: The invention relates to compounds which have an affinity for the ? opioid receptor and the ORL1 receptor, processes for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.