Abstract: The present invention belongs to the field of agricultural acaricides, and particularly relates to a trifluoroethyl thioether (sulfoxide) substituted benzene compound and use thereof. The compound has a structure as shown in general formula I: The definition of each substituent in the formula is described in the specification. The compound of general formula I has excellent acaricidal activity and can be used to prevent and control various pest mites.

Abstract: A resolution method of axial chiral enantiomers of lesinurad (2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetic acid) adopts inexpensive and readily available quinoline natural products and derivatives thereof, such as quinine, cinchonine, quinidine or cinconidine as resolving agents to react with lesinurad racemate in an organic solvent to form a salt, and the salt is dissociated by acidification so as to obtain optically pure (R)- or (S)-2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetic acid. The method can give axial chiral enantiomer of lesinurad in R configuration with a chiral purity ee of up to 100% and a total yield of 90% or more. The obtained axial chiral enantiomer of lesinurad in S configuration can reach a chiral purity ee of up to 99.9% and a total yield of 80% or more.

Abstract: The present invention provides an improved process for preparing 5-chloro-2-[(3,4,4-trifluoro-3-buten-1-yl)thio]-thiazole comprising reacting 2-[(3,4,4-trifluoro-3-buten-1-yl)thio]-thiazole with N-chlorosuccinimide (NCS) in the presence of water, the improvement comprising performing the step of reacting the compound of formula (II) with NCS in the presence of a reduced amount of water. The present invention provides an improved process for preparing 5-chloro-2-[(3, 4,4-trifluoro-3-buten-1-yl)thio]-thiazole comprising reacting 2-[(3, 4,4-trifluoro-3-buten-1-yl)thio]-thiazole with N-chlorosuccinimide (NCS) in the presence of water, the improvement comprising performing the step of reacting the compound of formula (II) with an excess molar amount of NCS.

Abstract: The present invention relates to processes and intermediates for preparing compounds of formula (IA), wherein R1, R4, R5, R6, and L1 are as defined herein. Compounds of formula (IA) have been found useful as EP4 receptor agonists useful in the treatment of glaucoma, osteoporosis, neuropathic pain, and related disorders.

Abstract: The invention relates to compounds, compositions and methods for activating, reactivating, reversing or preventing the deactivation of cholinesterases, such as acetylcholinesterase and butyrylcholinesterase.

Abstract: The present technology relates to synthesis of resveratrol compositions, in particular to methods of synthesizing resveratrol salicylates such as those formed through the activation of resveratrol and salicylic acid, and cosmetic and pharmaceutical compositions comprising the same.

Abstract: Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used.

Abstract: Provided is a method for industrially producing a triazolidinedione compound at a high purity and a high yield. A precipitation step for preparing a solution that contains a triazolidinedione compound represented by formula (1) and precipitating the triazolidinedione compound therefrom is performed. In this step, the pH of the solution is adjusted to 3.0 to 8.5 and the solution is prepared so as to contain 3-15 parts by volume of solvents for 1 part by mass of the triazolidinedione compound. (In the formula, R1 is a substituted or unsubstituted amino group-bearing organic group.

Abstract: The present disclosure provides MAT2A inhibitor compounds that are useful as therapeutic agents for treating malignancies, and wherein the compounds conform to general formula (IA): wherein RA, RB, RC, RD, and RE are defined herein.

Abstract: This invention relates to processes for the preparation of antiparasitic isoxazoline compounds enriched in an enantiomer using quinine-based chiral phase transfer catalyst. The invention also relates to novel quinine-based phase transfer catalysts and to a toluene solvent form of the isoxazoline compound of the invention.

Abstract: The present invention relates to stable amorphous form of sacubitril valsartan trisodium complex and its solid dispersion compounds, processes for their preparation and pharmaceutical composition comprising the same. The present invention also relates to an improved process for the preparation of sacubitril sodium and its use in the preparation of sacubitril valsartan trisodium complex.

Abstract: The present invention provides freebase and salt forms, and compositions and methods thereof, useful for treating various conditions in which aldehyde toxicity is implicated in the pathogenesis by the administration of small molecule therapeutics acting as a scavenger for toxic aldehydes.

Abstract: The present invention composition features pharmaceutically acceptable salts of psilocin and compositions thereof. The pharmaceutically acceptable salts of psilocin may be used to treat a disease or condition, such as a neurological injury, an inflammatory condition, chronic pain, or a psychological condition, in a subject in need thereof.

Abstract: The present invention relates to a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2?-methyl-1,1?-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-meth19243yloxime, and/or an active metabolite thereof having antagonist action at the oxytocin receptor and/or vasopressin V1a receptor, to processes for their preparation, pharmaceutical compositions containing them and their use.

Abstract: Disclosed herein is a compound of formula (I), which is ammonium salt of GW5074, wherein R1, R2, and R3 are independently hydrogen, alkyl, alkenyl, alkynyl, aryl, or heteroaryl; or R1, R2, R3 and the nitrogen are taken together to form a 6-membered heterocyclyl; and the alkyl, the alkenyl, the alkynyl, the aryl, the heteroaryl, or the 6-membered heterocyclyl is optionally substituted with at least one substituent selected from the group consisting of, —OH, —NH2, and —NRaRb, in which Ra and Rb are independently alkyl, aryl, or heteroaryl. Also disclosed herein is a pharmaceutical kit for the treatment of cancers. The pharmaceutical kit includes, a first formulation comprising a c-Raf inhibitor and a pharmaceutically acceptable carrier; and a second formulation comprising the compound of formula (I) and a pharmaceutically acceptable carrier. Also encompasses herein is a method of treating a subject having a cancer.

Abstract: The present application relates to compounds according to (Formula IA) or (Formula IB): or a pharmaceutically acceptable salt thereof. The compounds can be used as inhibitors of ROR? and are useful for the treatment of ROR? mediated diseases.

Abstract: Novel compounds having inhibitory activity on the formation of fungal hyphae and biofilms, and therapeutic formulations and methods based on the novel inhibitors.

Abstract: Salts of glycopyrrolate, including solid forms and formulations such as topicals thereof, are disclosed. Methods of making glycopyrrolate salts, including formulations such as topicals thereof, and methods of treating hyperhidrosis with salts of glycopyrrolate, and formulations such as topicals thereof, are disclosed.

Abstract: Salts of glycopyrrolate, including solid forms and formulations such as topicals thereof, are disclosed. Methods of making glycopyrrolate salts, including formulations such as topicals thereof, and methods of treating hyperhidrosis with salts of glycopyrrolate, and formulations such as topicals thereof, are disclosed.

Abstract: The present invention relates to an improved and efficient process for the synthesis of 2-[2-(1-chlorocyclopropyl)-3-(2-chlorophenyl)-2-hydroxypropyl]-2,4-dihydro-3H-1,2,4-triazole-3-thione, compound of formula (I) (Prothioconazole). The present invention more particularly relates to an improved process for manufacturing of 2-(1-chloro-cycloprop-1-yl)-3-(2-chloro phenyl)-2-hydroxy propyl-1-hydrazine (compound of formula III) and 2-[2-(1-chlorocyclopropyl)-3-(2-chlorophenyl)-2-hydroxypropyl]-1,2,4-triazolidine-3-thione (compound of formula II) which are mainly used for synthesis of Prothioconazole which is knows as an active compound with microbicidal fungicidal properties.