Abstract: Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein R1, R2, Ra, G, X, Y, Z, and n are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a compound described herein and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.

Abstract: The present disclosure relates to 4-Azaindazole compounds having the following structure: or a pharmaceutically acceptable salt thereof, for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a 4-azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

Abstract: The present invention, in one or more embodiments, comprises derivatives of 3-n-pentadecylcatechol (poison ivy urushiol saturated congener) and/or 3-n-heptadecyl catechol (poison oak urushiol saturated congener) as compositions for the prevention and/or prophylactic treatment of contact dermatitis caused by poison ivy and poison oak. The present invention is also directed towards processes for making such compounds. Disclosed are compounds which are effective for tolerizing and desensitizing a subject against allergens contained in plants of the Anacardiaceae and Ginkgoaceae families comprising urushiol esters of general formula (IA) [Formula should be entered here] tolerizing and desensitizing mammals, including humans, to allergens contained in plants of the Anacardiaceae and Ginkgoaceae families is attained by administering a formulation containing at least one urushiol ester compound.

Abstract: Described are coelenterazine analogs, methods for making the analogs, kits comprising the analogs, and methods of using the compounds for the detection of luminescence in luciferase-based assays with low backgrounds and enhanced signal-to-background ratios.

Abstract: The present invention provides an isothiocyanate compound and its application. The compound is an aryl-substituted isothiocyanate compound that has a structure of the general formula I. The isothiocyanate compound of the present invention has very good solubility in water, far better inhibitory activity for XPO1 protein than other non-aryl substituted congeneric compounds, little side effects, and good biological safety and bioavailability, and is quite suitable for clinical application. Therefore, the isothiocyanate compound would have tremendous potential market space and economic benefits.

Abstract: The present invention provides a method for producing an atropisomer of a pyrrole derivative having excellent mineralocorticoid receptor antagonistic activity, and an intermediate thereof. A method for producing an atropisomer of a pyrrole derivative using a compound represented by (B) [wherein R1 represents a C1-C4 alkyl group, and R2 represents a 2-hydroxyethyl group or a carboxymethyl group] as a production intermediate.

Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof: wherein R1, R2, R3, R4, R5, R6, Q1, Q2, Y1, and Y2 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.

Abstract: The present disclosure relates to nucleosides, such as compositions, and methods useful for treating retinal damage and/or retinal degradation/retinal degeneration, for inhibiting inflammasome activation by Alu RNA associated with a cell, for reducing ATP-induced permeability of a cell, for reducing an amount of mitochondrial reactive oxygen species in a cell, and for reducing an amount of mitochondrial reactive oxygen species in a cell. The present disclosure further relates to nucleosides, such as compositions, and methods for use in protecting an RPE cell and/or for treating, including prophylactic and therapeutic treatment, of conditions associated with retinal damage and/or degradation including, but not limited to, dry age related macular degeneration (AMD) and wet AMD, Alzheimer disease, various forms of arthritis, atherosclerosis, diabetes mellitus, chronic obstructive pulmonary disease, inflammatory bowel disease, and Duchenne muscular dystrophy.

Abstract: The present invention relates to a pharmaceutical combination for use in the treatment of squamous cell carcinoma, comprising a CDK inhibitor selected from the compounds of formula (I); or a pharmaceutically acceptable salt thereof and one or more antineoplastic agents selected from sorafenib, lapatinib, erlotinib, cisplatin, 5-fluorouracil, docetaxel or cetuximab or a pharmaceutically acceptable salt thereof. The said pharmaceutical combination exhibits synergy when used in the treatment of squamous cell carcinoma of head and neck (SCCHN). The invention also relates to a pharmaceutical composition comprising the said combination and a method for the treatment of squamous cell carcinoma of head and neck (SCCHN), using a therapeutically effective amount of said combination.

Abstract: The present invention is directed to benzamide-containing compounds of formula I or pharmaceutically acceptable salts thereof which inhibit the P2X7 receptor, and their use in the treatment of epilepsy.

Abstract: Embodiments described herein provide a compound that may be used in a variety of applications such as corrosion inhibition, additives for metalworking, mining reagents, epoxy curatives, emulsifiers, fuel or lubricant additives, surfactant manufacture, acid scavengers and asphalt additives. The compound has the following structure: where R1 is a methoxy group, R2, R3, R4 and R5 are independently a hydrogen atom or an alkyl group, and R6 is an aminomethyl group.

Abstract: This invention describes a method of conjugating a cell binding agent such as an antibody with an effector group (e.g., a cytotoxic agent) or a reporter group (e.g., a radionuclide), whereby the reporter or effector group is first reacted with a bifunctional linker and the mixture is then used without purification for the conjugation reaction with the cell binding agent. The method described in this invention is advantageous for preparation of stably-linked conjugates of cell binding agents, such as antibodies with effector or reporter groups. This conjugation method provides in high yields conjugates of high purity and homogeneity that are without inter-chain cross-linking and inactivated linker residues.

Abstract: The disclosure provides fumagillol type compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of using, e.g. in the treatment of obesity are provided.

Abstract: Disclosed herein are compounds of formula (I): wherein: the groups R1, R2, R3, R4, R5, R6, R7, R8, R1?, R2?, R3?, R4?, R5?, R6?, R7?, R8?, R1?, R2?, R3?, R4?, R5?, R6?, R7?, R8? are defined herein; and at least one of the following conditions is satisfied: two radicals from at least one of the four following pairs of radicals are not the same radical: R1? and R8?, R2? and R7?, R3? and R6?, R4? and R5?, and two radicals from at least one of the four following pairs of radicals are not the same radical: R1? and R8?, R2? and R7?, R3? and R6?, R4? and R5?.

Abstract: There is provided compounds of formula I, wherein R1, R2, R3 R4, R5, R6, R7a and R7b have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. CDK8 and/or Haspin kinase) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.

Abstract: A multifunctional broad spectrum antimicrobial composition is described. The composition can be incorporated into a wood preservative, or used as an additive to provide antimicrobial properties to water-based wood coatings. The composition is a concentrated water-miscible emulsion containing 3-iodo-2-propynyl N-butylcarbamate (IPBC), carbendazim (BCM) and propiconazole (PPCZ), and has antimicrobial activity against a wide variety of fungal organisms, including surface molds, blue stain fungi and wood rotting fungi. The composition can act as an in-can preservative and is useful for antimicrobial protection of wood and wood-based substrates.

Abstract: The present invention provides a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof or a solvate of these. A compound having Nrf2 activation ability is provided by the present invention.

Abstract: The invention comprises novel pyrazolyl derivatives of the general formula (I) Also described are processes for preparing the compounds of the formula (I). The compounds according to the invention are especially suitable for controlling insects and archnids in agriculture, and ectoparasites in veterinary medicine.

Abstract: Nucleophile-reactive sulfonated compounds used as precursors to (radio)labelled (bio)molecules are produced by pre-introduction of a nucleophilic compound R* through an unusual nucleophile-induced ring-opening reaction of the sultone moiety of the precursor. The precursors and compounds conform to respective formulae (Ip) and (I): Also disclosed are methods for producing these precursors and compounds, as well as for conjugation of these compounds with (bio)molecules, and to the drugs obtained by this method.

Abstract: The present invention relates to a method for synthesizing tetrahydroisoquinoline thiazolidine, which can be conducted under a relatively mild reaction condition and can rapidly synthesize tetrahydroisoquinoline thiazolidine.