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 relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.

Abstract: The compounds of formula (I) are derived from perhydroquinoline and perhydroisoquinoline and are useful as active pharmaceutical ingredients for the prophylaxis or treatment of diseases caused by 11-beta-hydroxysteroid dehydrogenase type I (11-beta-HSD1) enzyme-associated disorders, such as glaucoma, elevated ocular pressure, metabolic disorders, obesity, metabolic syndrome, dyslipidemia, hypertension, diabetes, atherosclerosis, Cushing's syndrome, psoriasis, rheumatoid arthritis, cognitive disorders, Alzheimer's disease or neurodegeneration.

Abstract: The present application discloses the use of the anti-malarial drug lumefantrine and related compounds in the treatment of cancer.

Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.

Abstract: Provided are methods for using bis-quaternary ammonium compounds to treat inflammatory pain, neuropathic pain and nociceptive pain.

Abstract: The invention provides a method, compounds and compositions for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or GIi gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula (I).

Abstract: A compound of Formula (1) or a salt thereof, methods for the preparation and use of such a compound, especially as an IAP inhibitor, and related compounds, compositions, and methods.

Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders.

Abstract: The invention relates to derivative compounds of partially-reduced isoquinoline with substitution of a sec-butyl group at position 3 with calpain inhibitor activity. The inventive compound comprises an ester or amide derived from (3-sec-butyl-1-oxo-2,3-dihydro-1H-isoquinolin-4-yliden)-acetic acid and (3-sec-butyl-1-thioxo-2, 3-dihydro-1H-isoquinolin-4-yliden)-acetic acid. Compounds having formula I or II can be used in the preventive or therapeutic treatment of a degenerative disease.

Abstract: Anti-infective and biofilm-inhibiting activities of aryl isoquinoline-derivatives of the general formulae 1 to 3 are described.

Abstract: The present invention is about the use of at least one epothilone or derivative thereof as an active ingredient for manufacturing a medicament for use in the treatment of disease(s) involving a neuronal connectivity defect, such as schizophrenia or autism.

Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.

Abstract: In one aspect, the present invention provides for a compound of Formula I in which the variable X1a, X1b, X1c, X1d, Q, A, R1, B, L, E, and the subscripts m and n have the meanings as described herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.

Abstract: This application provides a method for the use of select quaternary ammonium antagonists to alpha-7 nAChR for the treatment of cancer and HIV and AIDS.

Abstract: Provided are methods of modulating, treating, reversing and/or preventing pain using tetrakis quaternary ammonium compounds, especially regarding pain of central and/or peripheral origin and/or pain which is nociceptive, neuropathic, somatic, visceral, and/or inflammatory in nature.

Abstract: Genipin derivatives and pharmaceutical compositions thereof that inhibit the activity of uncoupling protein-2 (UCP2) and are useful in treating deficient first-phase insulin secretion, non-insulin dependent diabetes mellitus, and ischemia in a mammal are disclosed.

Abstract: Provided are bis-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders.

Abstract: A method for causing a permanent increase in the length and girth of a male subject's penis, the method comprising treatment comprising the step of (a) administering to the male an effective amount of a vasodilator selected from the group consisting of a vasodilator per se and compositions thereof comprising a pharmaceutically-acceptable diluent or carrier, to induce a cumulative prolonged engorgement of the subject's penis; and (b) repeating step (a) as necessary to cause the increase during the treatment. A potentiator which enhances the effect of the vasodilator may also be used.

Abstract: The present application discloses derivatives of 8-epiblechnic acid and use thereof in treating a disease related to endothelin receptor A or endothelin-1 (ET-1) over-expression, such as hypertension, cancer, atherosclerosis, and myocardial infarction.

Abstract: The present invention relates to substituted tetrahydroisoquinoline compounds of general formula (I), a process for their preparation, medicaments comprising said substituted tetrahydroisoquinoline compounds as well as the use of said substituted tetrahydroisoquinoline compounds for the preparation of medicaments, which are particularly suitable for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via 5-HT6 receptors.

Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.

Abstract: The invention is directed to pharmaceutical compositions comprising colored solutions, colored emulsions, or colored powders of injectable pharmaceuticals wherein said pharmaceuticals are selected from the group consisting of muscle relaxants, hypnotics, induction agents, and anticholinergics. The formulations of the present invention may all be colored using fluorescein. Different colors may be achieved by either varying the concentration of fluorescein, or by combining fluorescein with another dye. The invention is also directed to methods involving the use of said pharmaceutical compositions.

Abstract: Provided are tetrakis-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders.

Abstract: Use of Bis 1,2,3,4-tetrahydroisoquinoline derivatives represented by formula (I) as SK channel blockers and for the preparation of a medicament useful for the treatment of disorders of the central nervous system.

Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.

Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.

Abstract: Ansamycins and methods of preparing and using the same are described. At least some of these ansamycins exhibit one or more of improved aqueous formulation ability, chemical stability, and bioavailability. Some of the derivatives described are dimers. These and others described can include one or more solubilizing groups that have expected merit in rendering the overall compounds useful as drugs and prodrugs.

Abstract: N-n-Alkylation of nicotine converts nicotine from an agonist into an antagonist specifically for neuronal nicotinic acetylcholine receptor subtypes mediating nicotine-evoked dopamine release. Conformationally restricted analogs exhibit both high affinity and selectivity at this site, and are able to access the brain due to their ability to act as substrates for the blood-brain barrier choline transporter.

Abstract: The present invention relates to symmetric and asymmetric dimeric Dmt (2?,6?-ditnethyl) compounds and Dmt derivative compounds with dual ? and ? opioid receptor antagonist activity. Also, the present invention provides compositions comprising these compounds and it provides methods of using these compounds.

Abstract: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.

Abstract: The present invention provides an antiallergic latex or PVC product, which includes one or more natural antiallergic medicines selected from baicalin, matrine, liquorice saponin, tea polyphenol, arctigenin, oleanolic acid, tetrandrine, sodium ferulate, total alkaloid of asiatic moonseed rhizome, extraction of cortex dictamni radics, ginkgo bilobal A, total glycoside of Rhizoma Anemones flaccidae, extraction of engelhardtia chryolepis, magnolin, osthole, catechin. The latex or PVC products of the present invention are generally in the forms of glove or condom. The present invention solves the problem of hypersensitivity to condom or glove in prior arts by adding the natural antiallergic medicine into the matrix of latex or PVC.

Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as VEGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: The invention provides novel neuromuscular blocking agents, methods of using the neuromuscular blocking agents as well as reagents, methods and kits for reversing the effects of the neuromuscular blocking agents.

Abstract: The present invention provides compositions and methods for preventing, treating or reversing neuronal dysfunction in a mammal resulting from exposure to organophosphate nerve agents, organophosphate insecticides and incapacitating agents of the central nervous system (CNS); CNS injury, including traumatic brain injury, neurologic complications of cardiac surgery, perinatal asphyxia, and stroke, spinal cord injury, and peripheral nerve injury; and neuronal disorders associated with the loss of motor function including post-polio syndrome, amyotrophic lateral sclerosis, myasthenia gravis, Parkinson's disease and Rett syndrome; neurodegenerative disorders including Alzheimer's disease, mild cognitive impairment and schizophrenia; and cognitive impairment associated with aging.

Abstract: A process for preparing the [R-[R*,R*-(E)]]-2,2?-(1,8-dioxo-4-octene-1,8-diyl) bis(oxy-3,1-propanediyl)bis(1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-1-[(3,4,5-trimethoxyphenyl) methyl]isoquinolinium) dichloride, commonly known as mivacurium chloride, useful as short-duration neuromuscular blocking agent.

Abstract: The invention described herein relates to certain bicyclic heteroaromatic N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

Abstract: The invention pertains to substituted quinazoline and isoquinoline compounds that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which are selective inhibitors of PDE-10. The invention also relates to intermediates for preparation of said compounds; pharmaceutical compositions comprising said compounds; and the use of said compounds in a method for treating certain central nervous system (CNS) or other disorders.

Abstract: The invention relates to the use of chemical chelators for the preparation of a medicament for the reversal of drug-induced neuromuscular block, to a kit for providing neuromuscular block and its reversal, and to cyclophane derivatives having general formula (A) wherein R is (a), (b) or (c); or general formula (B) wherein X is (a), (b) or (d), or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to melanocortin receptor agonists of formula I, which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunction

Abstract: The present invention discloses a seven amino acid peptide (7AA) of bombesin. Methods for reducing the impairment respiratory tract mucosal immunity, reducing the rate of infection of the respiratory tract by pathogenic microorganisms and reducing the atrophy or dysfunction of the GALT comprising administering an effective amount of 7AA are also provided.

Abstract: The specification discloses a method for enhancing the inhibiting action of drugs against multidrug resistant cells, apparently by reversing or inhibiting the glycoprotein “pumps” associated with such cells.

Abstract: The specification discloses a method for enhancing the inhibiting action of drugs against multidrug resistant cells, apparently by reversing or inhibiting the glycoprotein “pumps” associated with such cells.

Abstract: The invention relates to pharmaceutical formulations and methods for preparing pharmaceutical formulations of histamine releasers. The present invention provides methods for determining the concentration of physiologically acceptable excipients for use in the formulations of the invention. The present invention also provides methods for suppressing pharmaceutically-induced histamine release by administering to an animal, the formulations of the present invention. A kit useful for preparing pharmaceutical formulations of histamine releasers is also provided.

Abstract: The present inventors revealed that non-steroidal anti-inflammatory drugs and muscle relaxants suppressed the expression of genes carried on viral vectors. These agents also suppressed viral vector cytotoxicity. The present invention provides a method for regulating the expression of genes carried on viruses by using non-steroidal anti-inflammatory drugs and/or muscle relaxants. The effect of these agents is reversible, and viral vector gene expression and cytotoxicity increased after termination of agent administration. The agents of the present invention are useful for regulating the expression of viral and therapeutic genes, and for suppressing viral vector cytotoxicity in gene therapy using viral vectors.

Abstract: This invention is directed to physiologically active compounds of formula (I) wherein represents a bicyclic ring system, of about 10 to about 13 ring members, in which the ring is an azaheterocycle, and the ring represents an azaheteroaryl ring, or an optionally halo substituted benzene ring; R1 represents hydrogen or a straight- or branched-chain alkyl group of 1 to about 4 carbon atoms, optionally substituted by hydroxy or one or more halogen atoms, or when Z1 represents a direct bond R1 may also represent a lower alkenyl or lower alkynyl group, or a formyl group; R2 represents hydrogen, alkenyl, alkoxy, alkyl, alkylsulphinyl, alkylsulphonyl, alkylthio, aryl, arylalkyloxy, arylalkylsulphinyl, arylalkylsulphonyl, arylalkylthio, aryloxy, arylsulphinyl, arylsulphonyl, arylthio, cyano, cycloalkenyl, cycloalkenyloxy, cycloalkyl, cycloalkyloxy, heteroaryl, heteroarylalkyloxy, heteroaryloxy, hydroxy, —SO2NR4R5, —NR4SO2R5, —

Abstract: Methods and compositions are provided for the effective treatment of macular degeneration. The methods relate to administering a treatment including an effective amount of a combination of polyvinyl pyrollidone, procaine and thiamine to a mammalian host.

Abstract: A method for optimizing pupil size in individuals suffering from excessive pupillary dilation in dim light as well as through medication is disclosed. Alpha 1 antagonist is applied in an eye drop formulation to the eye, resulting in reduced pupil size in dim light, but less reduction in pupil size in bright light.

Abstract: A novel solid pharmaceutical dispersion that improves the bioavailability of poorly water soluble drugs is produced by combining the drug with a polymer carrier such as polyvinylpyrrolidone. The drug is combined with the carrier without the need for using organic solvents or melting temperatures (fusion) through the use of a transition compound such as polyethylene glycol which partially solubilizes the drug and/or plasticizes the polymer.

Abstract: The use of diaryl acid derivatives of formula (I) or pharmaceutically acceptable salts, N-oxides, hydrates or solvates thereof, wherein the variables shown are defined in the disclosure, and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as agonists or antagonists of the PPAR receptor.