Abstract: The invention relates to pyrrolone compounds of the formula (I) wherein X, R1, R2, R3, Ra, Rb, Rc and Rd are as defined in the specification. Furthermore, the present invention relates to processes and intermediates for making compounds of formula (I), to herbicidal compositions comprising these compounds and to methods of using these compounds to control plant growth.

Abstract: The present invention relates to compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: each of A, B, C, D, and E, independently, is C, N, N—H, O, S, or absent is a single bond or a double bond; each of X, Y, and Z, independently, is aryl, heteroaryl, aralkyl, H, or absent; each of L1 and L2, independently, is a moiety selected from O, CH2, C?O, C2-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, —((CH2)n—W)—, wherein n=0, 1, 2, 3, 4, or 5, and W is O or S, or absent; and when L2 is absent, Z is aryl or heteroaryl fused with BC. Also provided in the present invention is a method for inhibiting, treating and/or reducing the risk of a neuropsychiatric disorder, comprising administering a subject in need a composition comprising a compound of Formula (I).

Abstract: The present application is directed to compounds of Formula I: compounds comprising these compounds and their uses, for example as medicaments for the treatment of diseases, disorders or conditions mediated or treatable by inhibition of binding between WDR5 protein and its binding partners.

Abstract: This invention relates to compounds of formula (I), a process for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions having an association with the orexin sub-type 1 receptor. Ar, R1, R2, R3, R4, R5, R6 and R7 have meanings given in the description.

Abstract: This invention relates to compounds of formula (I), a process for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions having an association with the orexin sub-type 1 receptor. Ar1 and Ar2 have meanings given in the description.

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, or a solvate thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.

Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1, or a salt thereof wherein Q, R1, R2, R3 and R4 are as defined herein.

Abstract: This invention relates to compounds of formula (I), a process for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions having an association with the orexin sub-type 1 receptor. Ar, R1, R2, R3, R4, R5 have meanings given in the description.

Abstract: This invention relates to compounds of formula (I) a process for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions having an association with the orexin sub-type 1 receptor. Ar, R1, R2 and R3 have meanings given in the description.

Abstract: The present invention relates to novel N-[(Pyrimidinylamino)propanyl]- and N-[(Pyridinylamino)propanyl]arylcarboxamide derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment or prevention of conditions having an association with the orexin sub-type 1 receptor.

Abstract: This disclosure provides a process for preparing 1-(arylmethyl)quinazoline-2,4(1H,3H)-diones, specially provides a method for preparing the compound of Formula I, and the method comprises the step of reacting the compound of Formula II with the compound of Formula A in the presence of a condensation agent, an organic base and an organic solvent by condensation.

Abstract: The present invention provides a novel crystalline form of Lumacaftor, specifically Lumacaftor Form APO-1, a co-crystal of Lumacaftor and nicotinamide, compositions including this crystalline form, and processes for the preparation of this crystalline form.

Abstract: The present invention relates to ampakines, including low impact ampakines, and pharmaceutical compositions and methods employing ampakines for treating central nervous system (CNS) disorders, including attention deficit disorders. Novel compositions and methods are provided employing anti-ADHD ampakines to treat attention deficit hyperactivity disorder (ADHD) and related cognitive, behavioral and psychiatric conditions.

Abstract: Provided are methods of treating and/or preventing dermatological disorders. Provided are methods of reducing skin inflammation, reducing pain, and/or reducing itch in a subject in need thereof. The methods may include administering to the subject an effective amount of a TRPV4 inhibitor. Further provided are compositions including a TRPV4 inhibitor compound in combination with a carrier, vehicle, or diluent that is suitable for topical application. Further provided is a transgenic mouse whose genome includes deletions of the Trpv4 gene in keratinocytes of the epidermis, wherein said transgenic mouse is a knockout for the Trpv4 gene in keratinocytes of the epidermis following keratinocyte-specific activation and expression of a site-specific recombination enzyme.

Abstract: The present invention encompasses compounds of the formula (I) wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.

Abstract: Compounds of formula I wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.

Abstract: Provided are compositions and methods for treating osteoarthritis including intra-articular administration of a compound of Formula (I) including amorphous and polymorph forms thereof.

Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the compounds of Formula (I) or (II), or compositions thereof, for treating or preventing a wide range of diseases (e.g., proliferative diseases (e.g., cancers, benign neoplasms, angiogenesis, inflammatory diseases, autoimmune diseases) and metabolic diseases (e.g., diabetes (e.g., type 2 diabetes, gestational diabetes)) in a subject. Treatment of a subject with a disease using a compound of Formula (I) or (II), or compositions thereof, may downregulate the expression and/or inhibit the activity of a kinase (e.g., a tyrosine kinase, such as a Tec kinase, in particular, bone marrow on X chromosome kinase (BMX)), and therefore, suppress tyrosine kinase singling in the subject.

Abstract: The invention relates to compounds of Formula (I): wherein R1, R2 and R3 are as defined in the description and claims, or pharmaceutically acceptable salts thereof, having ?v?6 integrin antagonist activity. The invention also relates to pharmaceutical compositions including a compound of Formula (I), or a pharmaceutically acceptable salt thereof, and to the use of a compound of Formula (I), or a pharmaceutically acceptable salt thereof in therapy, including in the treatment of a disease or condition for which an ?v?6 integrin antagonist is indicated, in particular the treatment of idiopathic pulmonary fibrosis.

Abstract: The present application provides bifunctional compounds of Formula (Ia) or (Ib): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which act as protein degradation inducing moieties for cyclin-dependent kinase 8 (CDK8). The present application also relates to methods for the targeted degradation of CDK8 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to CDK8 which can be utilized in the treatment of disorders modulated by CDK8.

Abstract: This invention discloses the use of aza-tryptanthrin derivatives as an IDO1 and/or TDO inhibitors, and the derivatives are represented by the general Formula (I). The compounds represented by the Formula (I) have inhibitory effects on indoleamine-2,3-dioxygenase 1 (IDO1) and/or tryptophan-2,3-dioxygenase (TDO), and can be used for treating diseases having the pathological features of IDO1 and/or TDO-mediated tryptophan metabolism, including but not limited to tumors, autoimmune disease, infectious diseases, Alzheimer's disease, depression, anxiety.

Abstract: The disclosure provides new, stable, pharmaceutically acceptable salt forms of 1-(4-fluoro-phenyl)-4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one, together with methods of making and using them, and pharmaceutical compositions comprising them.

Abstract: The disclosure provides new, stable, pharmaceutically acceptable co-crystal forms of 1-(4-fluoro-phenyl)-4-((6bR, 10aS)-3-methyl-2,3,6b,9, 10, 10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de[quinoxalin-8-yl)-butan-1-one, together with methods of making and using them, and pharmaceutical compositions comprising them.

Abstract: The invention provides compounds of Formula XXIII: wherein R1 is hydrogen, alkyl, acyl, or silyl, R2 is hydrogen, alkyl, benzyl, acyl, or ester, and R3 is hydrogen, alkyl, an aromatic group, azacyclic, carbocycle, aryl, cycloalkyl, heterocycloalkyl, heterocycle, heteroaryl, heteroalkyl, acyl, or ester, as well as derivatives and stereoisomers, pharmaceutically acceptable salts and derivatives thereof; and methods of making and using such compounds. The invention includes pharmaceutical compositions containing such compounds, and the use of such compounds in methods of treating conditions, diseases, or disorders.

Abstract: Disclosed herein are amido compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

Abstract: The present application provides salt forms of N-(4-(4-Amino-7-(1-isobutyrylpiperidin-4-yl)pyrrolo[1,2-f][1,2,4]triazin-5-yl)phenyl)-1-isopropyl-2,4-dioxo-3-(pyridin-2-yl)-1,2,3,4-tetrahydropyrimidine-5-carboxamide and N-(4-(4-Amino-7-(1-isobutyrylpiperidin-4-yl)pyrrolo[1,2-f][1,2,4]triazin-5-yl)phenyl)-1-isopropyl-2,4-dioxo-3-phenyl-1,2,3,4-tetrahydropyrimidine-5-carboxamide, which are useful as inhibitors of TAM kinases, as well as processes and intermediates related thereto.

Abstract: A series of fused pentacyclic imidazole derivatives, being potent modulators of f benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders. In particular, the present invention is concerned with 5,7,8,15-tetrahydro-6H-8,15- methanobenzimidazo[1,2-b][2,5]benzodiazocin-6-one derivatives and analogs thereof.

Abstract: The present invention provides the following compounds having anti-viral activity. A1 is CR1AR1B, S or O; A2 is CR2AR2B, S or O; A3 is CR3AR3B, S or O; A4 is CR4AR4B, S or O; the number of hetero atoms among atoms constituting the ring which consists of A1, A2, A3, A4, nitrogen atom adjacent to A1 and carbon atom adjacent to A1, is 1 or 2; R1A and R1B are each independently hydrogen, halogen, alkyl, or the like; R2A and R2B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B are each independently hydrogen, halogen, alkyl, or the like; R4A and R4B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B may be taken together to form non-aromatic carbocycle or non-aromatic heterocycle; X is CH2, S or O; R1 is each independently halogen, hydroxy, or the like; m is any integer of 0 to 2; and n is any integer of 1 to 2.

Abstract: The invention provides heterobicyclic pyrimidinone compounds such as thiazolo[3,2-a]pyrimidinone compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson's disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary heterobicyclic pyrimidinone compounds described herein include 5-oxo-2,3-dihydro-5H-hiazolo[3,2-a]pyrimidine-6-carboxamide compounds.

Abstract: The present application discloses compounds which are activators of autophagic flux and pharmaceutical compositions comprising said activators. It further discloses use of said compounds and pharmaceutical compositions in the treatment of neurodegenerative diseases, particularly proteinopathies and tauopathies such as Alzheimer's disease. It further discloses methods of enhancing autophagic flux.

Abstract: The present disclosure relates generally to compounds and compositions, and their use as kinase inhibitors.

Abstract: A fused polycyclic heteroaromatic compound represented by Chemical Formula 1, and an organic thin film, an organic thin film transistor, and an electronic device including the fused polycyclic heteroaromatic compound are provided. The fused polycyclic heteroaromatic compound may have a conjugation structure but reinforce planarity among adjacent rings and have further dense packing and thus much increase charge mobility.

Abstract: The invention relates to novel methods for preparing indolinobenzodiazepine dimer compounds and their synthetic precursors.

Abstract: The present invention discloses a silicon incorporated quinoline of formula (I) wherein, X, Y, A, R1 and R2 are as described. The present invention further discloses a process for the preparation of silicon incorporated quinolines of formula I; a pharmaceutical composition comprising silicon incorporated quinolines of formula (I) or pharmaceutically acceptable salt thereof. The present invention also discloses a method for treating diseases caused by Plasmodium falciparum or other coccidian parasites using the silicon incorporated quinolines of formula I or pharmaceutically acceptable salt thereof.

Abstract: A trisiloxane having at least one carbinol functional group comprises the reaction product of (A) an initial trisiloxane and (B) an organic compound. Component (A) has a pendant silicon-bonded functional group selected from a hydrogen atom, an epoxy-containing group, an ethylenically unsaturated group, and an amine group. Typically, component (A) is free of certain terminal silicon-bonded functional groups and is free of polyoxyalkylene groups. Component (B) has a functional group reactive with the pendant silicon-bonded functional group of component (A), and has at least one hydroxyl functional group. The trisiloxane is useful for a number of applications including use as a detergent additive. The trisiloxane may be of the following general formula (I): (R13SiO1/2) (R1R3Si2/2)(R13SiO1/2) (I). In formula (I), each R1 is an independently selected hydrocarbyl group. R3 may be selected from the groups (i) to (iv) described herein. Typically, the trisiloxane has 1-6 carbinol groups.

Abstract: A process can prepare a colourless, methanolic solution of 3-(N-benzyl-2-aminoethyl)aminopropyltrimethoxysilane hydrochloride. The process includes, in step 1 fractionally distilling the vinylbenzyl chloride reactant component with addition of at least one stabilizer, and in step 2, metering and mixing the distillate (vinylbenzyl chloride) from step 1 into an initial charge of N-(2-aminoethyl)-3-aminopropyltrimethoxysilane and methanol in a molar ratio of the N-(2-aminoethyl)-3-aminopropyltrimethoxysilane to vinylbenzyl chloride of 1.0:0.80 to 1.0:1.15 and at a temperature in the range from 40 to 60° C. and leaving them to react further. The colourless, methanolic solution has an APHA colour number of <200 mg Pt—Co/I.

Abstract: An organometallic compound represented by Formula 1: M(L1)n1(L2)n2(L3)n3??Formula 1 wherein in Formula 1, M, L1, L2, L3, n1, n2, and n3 are the same as defined in the specification.

Abstract: Unsymmetrical metallocene compounds based on cyclopentadienyl ligands are disclosed, as well as catalytic compositions comprising the compounds supported on solid support materials. The compounds and compositions are useful as catalysts in the polymerisation of olefins. In particular, the compounds and compositions are useful catalysts in the preparation of low molecular weight polyethylene (e.g. polyethylene wax) and copolymers formed from the polymerisation of ethylene and other ?-olefins.

Abstract: A composition, and a crocins active site extracted from Gardenia jasminoides Ellis, mainly comprising the following ingredients: crocetin di-?-D-gentiobioside, crocetin-?-D-glucopyranosyl-?-D-gentiobioside, crocetin di-?-D-glucopyranoside, 13Z-crocetin di-?-D-gentiobioside, neocrocin B, crocetin mono-?-D-gentiobioside, 13Z-crocetin-8-O-?-D-gentiobioside, 13Z-crocetin-8?-O-?-D-gentiobioside, and crocetin mono-?-D-glucopyranoside. Pharmacological experiment results show that the crocins active site can effectively improve learning and memory injuries in mice induced by scopolamine and amyloid ? protein.

Abstract: Provided are a new crystal form of fludarabine phosphate, a preparation method therefor, a pharmaceutical composition containing same, and an application thereof in preparing medicine. Crystal forms I and II of the fludarabine phosphate have excellent properties in terms of solubleness, dissolution rate, chemical stability, and processing adaptability.

Abstract: The present disclosure relates to photoactivable protecting groups containing a diarylsulfide chromophore, a method for the synthesis thereof and their use as photoactivable protecting groups using maskless photolithography based array synthesis.

Abstract: A method of functionalizing RNA in a liquid sample includes reacting an anhydride function of a binding molecule with at least one RNA molecule at one or more hydroxyl groups in any of position 2? of a ribose of any nucleotide of the RNA molecule, position 2? of the ribose of the terminal nucleotide at the 3? end of the RNA molecule, or position 3? of the ribose of the terminal nucleotide at the 3? end of the RNA molecule, to obtain functionalized RNA. The binding molecule includes an aza-isatoic anhydride or derivative thereof linked to a group of interest by a linkage, and an aza-anthranilate is formed from reacting the anhydride function of the binding molecule with a hydroxyl group of the RNA molecule so as to join the RNA molecule to the group of interest. The group of interest is a marker, labelling precursor, or ligand.

Abstract: Probe embodiments for targeting, identifying, and isolating enzymes exhibiting BSH activity as well as devices and kits that use the probes are described herein. Methods of making and using the probes, devices, and kits are also described. In some embodiments, probes, devices, and kits for targeting, identifying, and isolating enzymes in a biological sample are disclosed. In some embodiments, compositions and methods of treatment using the probes, devices, and kits disclosed herein are described.

Abstract: Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I): and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, tinnitus, status epilepticus.

Abstract: An efficient tool with low cost to rapidly isolate and concentrate the secreted proteins of microorganisms in high quality. By this device, the secreted proteins are concentrated by passing through a dialysis membrane at electrophoretic conditions.

Abstract: The present invention provides compounds that can modulate opioid receptors. Some compounds of the invention are modulators of ?- and/or ?-opioid receptors. Still other compounds of the invention are opioid receptor antagonists. Some compounds of the invention can modulate opioid receptors with a significantly less likelihood of developing addiction or abuse compared to conventional opioid ligands, such as morphine. In particular, compounds of the invention are of the formula: wherein Ar1 is H, optionally substituted aryl or optionally substituted heteroaryl; R1 is a heteroalkyl; R2 is alkyl; R3 is an oligopeptide or a moiety of the formula —R4—Y; R4 is alkylene; Y is optionally substituted heteroaryl, optionally substituted aryl or a moiety of the formula —C(?X2)—X3—R5; each of X1, X2 and X3 is independently O, NR6 or S; and each of R5 and R6 is independently H or alkyl.

Abstract: The invention relates to the synthesis of boronic ester and acid compounds. More particularly, the invention provides improved synthetic processes for the large-scale production of boronic ester and acid compounds, including the peptide boronic acid proteasome inhibitor bortezomib.

Abstract: Antimicrobial molecules, their synthesis and use as antimicrobial treatments are described. The antimicrobial compounds are teixobactin analogues. Methods of synthesizing antimicrobial teixobactin analogues are also provided. Antibiotic therapeutics comprising antimicrobial teixobactin analogues are provided, along with methods of and formulations for treating microbial infections using such antimicrobial teixobactin analogues. Prodrugs formed using esterified forms of antimicrobial teixobactin analogues may also be provided.

Abstract: Provided is a novel peptide for skin regeneration or wound healing and a use thereof. The novel peptide not only promotes the wound healing by increasing the production amount of collagen in dermal fibroblasts but also has an excellent whitening effect by inhibiting the production amount of melanin and tyrosinase activity of melanoma cells, and consists of peptides having a very small size to minimize side effects according to administration of external substances of very small peptides. As a result, it is expected that the novel peptide can be used as an active substance that can replace existing skin regeneration or would therapeutic agents.

Abstract: Provided is a novel peptide for preventing or treating inflammatory diseases and a use thereof. According to the novel dimeric or trimeric peptide, it is possible to not only exhibit an excellent therapeutic effect through anti-inflammatory action but also have a very small-sized peptide, thereby minimizing side effects due to the administration of external substances. Therefore, it is expected that the peptide can be used as an active substance that can replace existing therapeutic agents for inflammatory diseases.