Abstract: The present invention relates to arylamide derivatives having dual pharmacological activity towards both the ?2? subunit, in particular the ?2?-1 subunit, of the voltage-gated calcium channel and the ?-opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.

Abstract: A method for producing a saccharified solution making it possible that while the concentration of a solid in a reactor is kept high at an initial stage of hydrolyzing a cellulose contained in a biomass with an enzyme, the biomass is earlier solubilized to be made into a slurry form. In the method, at an initial stage of mixing an aqueous solution containing a biomass pulverized in a reactor, the aqueous solution is poured into reactor, and then pulverized biomass is supplied thereinto step by step while content in reactor is stirred. A final solid concentration in reactor is set into the range of 15 to 30% both inclusive by mass. The reactor's bottom plane is made into a conical or mirror plate form. At least in upper and lower parts of the reactor's inside, plural stirring fans having a long rotation radius are located to stir content in reactor.

Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar1, R1, R2, R3, R4, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

Abstract: The disclosure relates to Prostaglandin receptor EP2 antagonists, derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing conditions and diseases in which EP2 receptor activation has a physiological role, such as but not limited to, brain injury, inflammatory diseases, neuroinflamation after a seizure, pain, endometriosis, cancer, rheumatoid arthritis, skin inflammation, vascular inflammation, colitis, and neurological disorders by administering a pharmaceutical composition comprising a compound disclosed herein to a subject in need thereof.

Abstract: The present invention relates to reduction of erythrocyte sedimentation rate in a blood sample. In particular, formulations, compositions, articles of manufacture, kits and methods for reduced erythrocyte sedimentation rate in a blood sample are provided.

Abstract: An object of the present invention is to provide a fluorescent probe that easily penetrates a cell and is capable of selectively and efficiently detecting singlet oxygen generated in the cell, a singlet oxygen detection agent containing the fluorescent probe, and a singlet oxygen detection method using the fluorescent probe. The fluorescent probe for detecting singlet oxygen comprises a compound having a silicon-rhodamine skeleton and a skeleton that increases the fluorescence of the fluorescent probe after trapping singlet oxygen to be greater than the fluorescence before trapping singlet oxygen, or a salt, hydrate, or solvate thereof.

Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.

Abstract: The present invention provides a method to produce RD by using a cutinase to catalyze the esterification of RB under stepwise cooling temperatures, which is related to the field of biosynthesis of organic compounds. The method uses a cutinase from Thermobifida fusca to catalyze the esterification of RB and sophorose to produce RD. The stepwise cooling temperatures are used to reduce the heat inactivation of the enzyme as well as to improve the mass transfer. The method catalyzes the esterification of RB to produce RD in a solvent such as methanol, DMSO and DMF. The reaction is safe, efficient and highly selective. In addition, the method uses stepwise additions of substrate RB and cooling temperatures for the esterification reaction. In this way, it speeds up the initial reaction rate, increases the amount of solved RB as it is converted to RD, and improves the mass transfer to further increase the reaction speed.

Abstract: Tetrahydroquinoline sulfonamide derivatives of formula (I), the pharmaceutically acceptable addition salts thereof, the hydrates and/or solvates thereof, and the use of same as inverse agonists of retinoid-related orphan receptor gamma (ROR?t) are described. Pharmaceutical compositions including such compounds, as well as the use thereof for the topical and/or oral treatment of ROR?t receptor-mediated inflammatory diseases, in particular acne, psoriasis and/or atopic dermatitis are also described.

Abstract: The invention relates to compounds of formula (I): wherein Q, A1, A2, A3, A5, A6, A7, A8, R4a, R4b and R5 are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.

Abstract: Provided herein are tricyclic small molecule inhibitors of maternal embryonic leucine zipper kinase (MELK). The compounds are useful for treating cancer and other conditions or diseases associated with aberrant MELK expression. Also provided herein are pharmaceutical compositions comprising a tricyclic compound of the invention and a pharmaceutically acceptable carrier. The invention also provides methods of treating cancers associated with over-expression of MELK.

Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.

Abstract: The present disclosure relates to the use of GnRH receptor antagonists used in the treatment of endometriosis or uterine fibroids. In particular, the present disclosure describes a method of treating endometriosis or uterine fibroids, where the method involves the administration of elagolix, and where the method may further involve the co-administration of rifampin or ketoconazole.

Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.

Abstract: The present invention provides methods and uses of inhibitors of histone deacetylase 11 (HDAC11) in the treatment of diseases and/or disorders, such as, for example, cell proliferative diseases.

Abstract: An antibiofilm composition comprising a compound of formula (A1), (A2) or (A3): wherein each of R1, R2, R3, R4, R5, R6 and R7 is independently selected from hydrogen, alkyl, alkenyl, aryl, halo, alkoxy, hydroxyl, amino, nitro, sulfoxy, thiol, carboxy, alkyl carboxy and amido; and X may be O or S, wherein the composition does not comprise a compound of formula (B1) or (B2):

Abstract: The novel bisphosphonic acid ester derivatives represented by the following formula (1): Y—Cy—(NH)m—(CH2)n—C(X)(PO(OR1)(OR2))2??(1) wherein each symbol is as defined in the DESCRIPTION, which has an amino group substituted by a heterocyclic group or a heterocyclic group containing a nitrogen atom, and the acid moiety is esterified with a POM group, an n-butanoyloxymethyl (BuOM) group and the like, exhibit a superior direct or indirect cytotoxicity effect on tumor cells and virus infected cells.

Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.

Abstract: Disclosed herein are spirocyclic compounds, together with pharmaceutical compositions and methods of ameliorating and/or treating a cancer described herein with one or more of the compounds described herein.

Abstract: The present invention relates to materials and methods for high throughput monitoring of target engagement of isopeptidases, such as deubiquitylating enzymes by, inter alia, small molecule inhibitors. In particular the invention relates to development of high throughput assays to measure isopeptidase activity in biological samples, such as cells, animal tissues, animal tumours, human tissue or patient-derived biopsies.