Abstract: Tricyclic indazole compound and its pharmaceutically acceptable salts of acid addition, use thereof, method and intermediates for preparing them, and a pharmaceutical composition containing them. The tricyclic indazole compound has the following general formula (I): in which R1, R2, L1, L2, X1, X2, X3, X4, X5, Y, W, m, and n have the meanings stated in the description.

Abstract: The present invention provides an antitumor effect potentiator for enhancing antitumor activity of an antitumor agent comprising tegafur in a therapeutically effective amount, gimeracil in an amount effective for enhancing an antitumor effect, and oteracil potassium in an amount effective for inhibiting a side effect. The antitumor effect potentiator comprising at least one member selected from the group consisting of folinic acid and pharmacologically acceptable salts thereof. The present invention also provides a method for enhancing an antitumor effect of an antitumor agent comprising the step of administering to a patient the aforementioned antitumor effect potentiator; and a method for cancer treatment comprising the step of administering to a patient the aforementioned antitumor agent.

Abstract: The present invention provides an integrase inhibitor. The inventors have found the following compound of formula (I) possessing an integrase inhibitory activity. (wherein, RC and RD taken together with the neighboring carbon atoms form a ring which may be a condensed ring, Y is hydroxyl, mercapto or amino; Z is O, S or NH; RA is a group shown by (wherein, C ring is N-containing aromatic heterocycle) or the like).

Abstract: Benzofuran compound, composition thereof, kit thereof, and/or method thereof. A benzofuran-2-carboxamide moiety may be N-arylated and/or N-alkylated, and the resulting benzofuran compound may be a sigma receptor ligand that binds to, e.g., a ?1 receptor and/or a ?2 receptor with relatively high affinity and/or selectivity. For example, the benzofuran compound may be 5,6-dimethoxy-3-methyl-N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamide, 3-methyl-N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamide, or 6-methoxy-3-methyl-N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamide. The composition may include the benzofuran compound and a pharmaceutically acceptable carrier.

Abstract: The present invention provides a new crystalline form VII of agomelatine, its method of preparation, application and pharmaceutical composition. This new crystalline form offers high purity, a stable crystalline structure and good reproducibility, while its method of production lends itself well to large scale production. In terms of stability and purity, it is superior to the numerous crystalline forms which have hitherto been reported. As a result, the crystalline form VII of the present invention possesses advantages in pharmaceutical preparation.

Abstract: Embodiments of the invention are directed to identifying or treating a patient that would benefit from phosphodiesterase inhibitor therapy.

Abstract: The present invention describes new amino pyrimidine derivatives and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel amino pyrimidines may be effective in the treatment of autoimmune disorders, inflammatory diseases, allergic diseases, airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), transplant rejection, cancers e.g. of hematopoietic origin or solid tumors.

Abstract: The present invention provides drug therapy formulations. In some embodiments, the present invention provides combinations of pharmaceutical agents (e.g., stimulant and non-stimulant), pharmaceutical formulations (e.g., nanoparticualte, non-nanoparticualte, etc.), and release profiles (e g, immediate release, delayed release, sustained release, etc.) to provide therapeutic benefit with reduced side effects.

Abstract: The present invention provides solid state forms of Vilazodone and Vilazodone hydrochloride, processes for preparing these solid state forms, and pharmaceutical compositions comprising one or more of these solid state forms.

Abstract: The present invention relates to methods for treating an ophthalmic, otic, or nasal infection comprising treating the infected tissue with a suspension composition comprising finafloxacin or a finafloxacin derivative. The present invention also relates to antimicrobial compositions comprising finafloxacin free base or a finafloxacin derivative. The compositions are suitable for the treatment of ophthalmic, otic, or nasal infections.

Abstract: Methods are provided herein for treating an individual having a disease, disorder or condition affecting the lungs, wherein said disease, disorder, or condition of the lung is an acute lung injury. In specific embodiments, the acute lung injury is chemical induced acute lung injury (CIALI). In some embodiments, the methods are provided for treating or protecting a subject from chemical induced acute lung injury that include administering to the subject a therapeutically effective amount of a phosphatase located on chromosome 10 (PTEN) inhibitor such as N(9,10-dioxo-9,10-di-hydrophenanthren-2-yl)pivalamide (SF1670). In some embodiments, the method products a subject from CAILI or reduces CAILI that results from a subsequent exposure to a chemical that induces chemical induced acute lung injury.

Abstract: A method for highly efficiently preparing high purity crystals of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chloro-phenyl]-ethyl]-1,3-propanediol hydrochloride. The method involves dissolving 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol in a mixed solvent comprising a solvent in which its hydrochloride is highly soluble and a solvent in which its hydrochloride is less soluble, to prepare a solution of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol; and then adding hydrochloric acid to the resulting solution with stirring, to crystallize the hydrochloride of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chloro-phenyl]ethyl]-1,3-propanediol.

Abstract: The present invention provides a compound having a PDE2A selective inhibitory action, which is useful as an agent for the prophylaxis or treatment of schizophrenia, Alzheimer's disease and the like. The present invention is a compound represented by the formula (1): wherein each symbol is as described in the specification, or a salt thereof.

Abstract: Disclosed is a method of inducing and promoting development of beneficial gut flora in a subject and/or of reducing the frequency and duration of crying periods in a subject, the method comprises administering to the subject a lipid composition comprising a vegetable-derived fat source, wherein the fat source is a triglyceride fat source comprising triglycerides with 15-55% palmitic acid moieties out of the total fatty acids, and wherein the level of palmitic acid moieties at the sn-2 position of the glycerol backbone is at least 30% of total palmitic acid. The method is particularly intended for children. Specific fat sources, as well as food articles and a commercial package comprising the same are disclosed.

Abstract: The present invention relates to the use of a compound of formula (I) wherein R1 and R3 are as defined in the description and R2 is a phenyl group which is substituted with 2 or 3 C1-C6 alkoxy groups, or a physiologically acceptable salt thereof, or a solvate of the compound of formula (I) or of the salt thereof, for treatment of colorectal or gastric adenocarcinoma.

Abstract: The present invention discloses a use of hesperetin or a hesperetin-containing plant extract in the manufacture of a product for improving and/or promoting skin microcirculation, or for eliminating and/or alleviating diseases or conditions associated with poor skin microcirculation. The present invention also discloses a composition comprising an effective amount of hesperetin or a hesperetin-containing plant extract, and to a method for improving and/or promoting skin microcirculation, or eliminating and/or alleviating diseases or conditions associated with poor skin microcirculation, by using hesperetin. The skin microcirculation of the present invention is preferably eye skin microcirculation.

Abstract: The present invention relates to compounds of the formula (I) and in particular medicaments comprising at least one compound of the formula (I) for use in the treatment and/or prophylaxis of physiological and/or pathophysiological states in the triggering of which cathepsin D is involved, in particular for use in the treatment and/or prophylaxis of arthrosis, traumatic cartilage injuries, arthritis, pain, allodynia or hyperalgesia.

Abstract: A composition for treating or preventing glaucoma or ocular hypertension including a isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate and a beta-receptor antagonist, in a combined pharmaceutically acceptable amount. As for the administration form, these drugs may be administered concomitantly or may be administered as a combination drug.

Abstract: The present invention relates to a compound of formula (I): The compound has apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and is thus useful in the treatment of diseases such as kidney disease, diabetic nephropathy and kidney fibrosis.

Abstract: A photopolymerizable dental composition for application to and for the isolation and protection of gums and/or teeth during dental treatment is described. The composition can include (a) one or more photopolymerizable monomers selected from the group consisting of acrylates and methacrylates, (b) one or more photoinitiators, preferably selected from the group consisting of alpha-diketones, benzoin alkyl ethers, thioxanthones, benzophenones, acyl phosphine oxides, acetophenones, ketals, titanocenes, borates and sensitizing dyes, and (c) one or more molecular weight regulators selected from the group consisting of compounds which can be reacted with a radical of a monomer of component (a) with abstraction of an H radical from the molecular weight regulator in the allyl position. Also disclosed are kits comprising such a composition, methods for producing a corresponding protective layer, methods for treating one or more teeth, and methods of using the compositions as a masking compound.