Abstract: An object of the present invention is to provide a novel integrase inhibitor. The present invention relates to a novel compound having an antiviral effect, more specifically, a pyridone derivative having HIV integrase inhibitory activity, and a medicament containing the same, in particular, an anti-HIV agent. The compound of the present invention has integrase inhibitory activity and/or cell proliferation inhibitory activity against viruses, in particular, HIV and drug-resistant strains thereof. Thus, the compound is useful in preventing or treating various diseases, viral infections (for example, AIDS), and the like in which integrase participates.

Abstract: A composition for regulating male sexual function includes at least one amino acid selected from a group consisting of L-Glutamic acid (glutamate), L-Arginine, glycine, L-aspartate, L-carnitine, L-tyrosine, L-glutamine and/or its pharmaceutically acceptable salt, such as any of monosodium-L-glutamate monogidrate, L-potassiumarginine, L,-ammoniumaspartate, L-arginine HCl, sodium-L-tyrasine, lithium aspartate, in the amount of 1-1000 mg, preferably 10-300 mg; at least one vitamin, in the amount of 1-500% of a daily recommended dose, preferably 10-200%; and at least one chelated compound of a formula: acid-Me-acid.nH2O, wherein Me is a metal chosen from any of Ca, Mg and Zn, wherein the acid is a dicarboxylic acid anion chosen from the group consisting of succinic acid, fumaric acid or aspartic acid, and wherein n=0-8. The composition increases testosterone level in a body of a male mammal.

Abstract: The present invention is directed to an implantable drug depot useful for reducing, preventing or treating post-operative pain in a patient in need of such treatment, the implantable drug depot comprising a therapeutically effective amount of clonidine or pharmaceutically acceptable salt thereof and a polymer; wherein the depot is implantable at a site beneath the skin to reduce, prevent or treat post-operative pain, and the depot is capable of releasing (i) about 5% to about 45% of the clonidine or pharmaceutically acceptable salt thereof relative to a total amount of the clonidine or pharmaceutically acceptable salt thereof loaded in the drug depot over a first period of up to 48 hours and (ii) about 55% to about 95% of the clonidine or pharmaceutically acceptable salt thereof relative to a total amount of the clonidine or pharmaceutically acceptable salt thereof loaded in the drug depot over a subsequent period of at least 3 days.

Abstract: The present invention is directed to a compound represented by the following structural formula or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions and method of use of the compounds are also described.

Abstract: A composition is provided having nano technological delivery of a medicament through the skin. The composition contains hydrocortisone, resveratrol and a sulfate free surfactant. The composition is formulated into a shampoo and the shampoo facilitates nano technological delivery of the hydrocortisone and the resveratrol through the skin of a user.

Abstract: A pharmaceutical combination comprising an EGFR inhibitor and an Hsp90 inhibitor according to the following formulae (I) or (Ia) a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables in the structural formulae are defined herein. Also provided are methods for treating a proliferative disorder in a subject in need thereof using pharmaceutical combinations disclosed herein.

Abstract: Thiazolylphenyl-benzenesulfonamido derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

Abstract: Treatment of patients with the 2S,4R ketoconazole enantiomer or its pharmaceutically acceptable salts, hydrates, and solvates is useful for reducing systemic inflammation and cholesterol levels and improving glycemic control.

Abstract: The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.

Abstract: Novel compounds for the treatment of estrogen receptor-mediated disorders, including breast cancer, and methods of treatment using the novel compounds. The novel compounds, when administered in a safe and effective amount, present extended binding to estrogen receptors in breast tissue without activating the estrogen receptors. Estrogen is blocked from binding to the estrogen receptors for an extended period of time, effectively hindering growth of breast cancer cells.

Abstract: The present disclosure is directed to chemically-stable and pharmaceutically acceptable sildenafil oral spray formulations for the treatment of diseases such as pulmonary arterial hypertension and/or SSRI-induced sexual dysfunction, wherein the oral spray formulation has a pH of about 1.5 to less than 3.0. The present disclosure is also directed to methods for treating diseases such as pulmonary arterial hypertension and/or SSRI-induced sexual dysfunction.

Abstract: Peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH) are provided. The compounds can suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS). Despite their relative inability to access brain and spinal cord, the compounds attenuate behavioral responses indicative of persistent pain in rodent models of inflammation and peripheral nerve injury, and suppresses noxious stimulus-evoked neuronal activation in spinal cord regions implicated in nociceptive processing. CBi receptor blockade prevents these effects. Accordingly, the invention also provides methods, and pharmaceutical compositions for treating conditions in which the inhibition of peripheral FAAH would be of benefit. The compounds of the invention are according to the formula (I): in which R1 is a polar group. In some embodiments, R1 is selected from the group consisting of hydroxy and the physiologically hydro lysable esters thereof.

Abstract: This invention relates to stable pharmaceutical compositions of 5,10-methylene-(6R)-, -(65)- or -(6R,S)-tetrahydrofolate (MTHF), by adjusting to a basic pH and the simultaneous use of citrate. Stabilisation is effected even in the absence of a reducing agent. The present invention is particularly suitable for producing lyophilisation solutions and lyophilisates or dry powders and dry mixtures, since the stable MTHF solutions can be used in high concentrations for filling corresponding vessels such as vials, ampoules, etc. The lyophilisates have a surprisingly long shelf life and are surprisingly stable. They can be reconstituted without problems by adding water or aqueous solutions, and the final clear injection solutions again exhibit excellent stability properties. Moreover, the present invention even makes it possible to prepare difficultly soluble calcium 15 or acidic salts of MTHF in high concentrations and as physiologically compatible isotonic solutions.

Abstract: The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.

Abstract: The present invention provides improved formulations of 6-mercaptopurine that exhibit better bioavailability and faster dissolution than previous formulations.

Abstract: The present invention relates to novel active substance combinations which contain firstly at least one known compound of the formula (I) in which R1 and A have the meanings given in the description, and secondly at least one further known active substance from the class of the macrolides, the carboxylates or other classes, and which are highly suitable for controlling animal pests such as insects and undesired acarids.

Abstract: The invention relates to novel pyrrolidine derivatives of formula (I): wherein R1, R2 and R3 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.

Abstract: Compounds active on the receptor protein tyrosine kinases c-kit and/or c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or conditions and/or c-fms-mediated diseases or conditions, and methods for the use thereof.

Abstract: This invention relates to a composition that comprises inositol phosphates and/or bisphosphonates, and to the use thereof to prevent the loss of substances of biological interest in the body of patients subjected to dialysis and to maintain sufficient physiological levels of said substances to regulate physiological and/or pathological processes, these substances being inhibitors of pathological crystallization.

Abstract: A montelukast composition having a therapeutically effective amount of montelukast in a sustained release is disclosed. A montelukast composition having a therapeutically effective amount of montelukast in an immediate release and sustained release is also disclosed.