Abstract: The invention relates to a compound of following formula (I): a preparation process, uses thereof and compositions containing the same, wherein R1 and R2, represent, independently of one another, a linear, branched or cyclic, saturated or unsaturated hydrocarbon-based group comprising from 1 to 6 carbon atoms, where the sum of the carbon atoms of the groups R1 and R2 ranges from 2 to 7, and where R1 and R2 may also form, together and with the carbon atom bearing them, a 6-, 7-, or 8-membered ring; n is an integer of between 1 and 100, limits included; A represents a sequence of one or more units chosen from ethylene oxide, propylene oxide, butylene oxide units and mixtures thereof; the group formed by R1, R2 and the carbon atom to which R1 and R2 are attached has a degree of branching equal to 0, 1 or 2.

Abstract: The present application pertains to processes producing oxides using a weak acid intermediate. In one embodiment a material comprising calcium carbonate is reacted with a solution comprising aqueous carboxylic acid to form a gas comprising carbon dioxide and a solution comprising aqueous calcium carboxylate. The solution comprising aqueous calcium carboxylate is reacted with sodium sulfate to form a solution comprising aqueous sodium carboxylate and a solid comprising calcium sulfate. The solution comprising aqueous sodium carboxylate is reacted with sulfur dioxide to form sodium sulfite and an aqueous carboxylic acid. The sodium sulfite is separated from said aqueous carboxylic acid and reacted to form a solid comprising calcium sulfite which is decomposed to form calcium oxide and sulfur dioxide.

Abstract: The present invention relates to a method for isomerizing a 3-(Z)-unsaturated carboxylic acid of the formula 1-Z or a salt thereof, wherein R2 is C1-C24-alkyl, C2-C24-alkenyl having 1, 2, 3 or more than 3 C—C double bonds, unsubstituted or substituted C5-C12-cycloalkyl, or unsubstituted or substituted aryl; R1 is hydrogen or has one of the definitions specified for R2; with the proviso that R2 has a higher priority than R1 in accordance with IUPAC; to give a 3-(E)-unsaturated carboxylic acid of the formula I-E or a salt thereof, wherein the isomerization of the compound of the formula 1-Z is effected in the presence of an anhydride of an organic acid and a base or in the presence of a ketene of formula CR11R12C(0), wherein R11 and R12 are as defined in the claims and in the specification and a base.

Abstract: The present invention relates to the compound (4,5,5-trimethyl-3-methylenecyclopent-1-en-1-yl)methyl acetate and to an attractant composition for insects of the species Delottococcus aberiae comprising said compound. The present invention also relates to an attractant device for Delottococcus aberiae comprising said compound or said composition, and to a method for the control and/or monitoring of the populations of insects of the species Delottococcus aberiae.

Abstract: A process to produce N-vinyl compounds by homogeneous catalysis can be performed. Acetylene is reacted with a compound having at least one nitrogen bearing a substitutable hydrogen residue in a liquid phase in the presence of at least one phosphine as a catalyst to produce the compounds.

Abstract: The present invention relates to mono- or di-substituted indole compounds, methods to prevent or treat dengue viral infections by using the compounds and also relates to use of the compounds as a medicine, more preferably for use as a medicine to treat or prevent dengue viral infections. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of dengue viral infections. The invention also relates to processes for preparation of the compounds.

Abstract: Crystalline hydrobromide salt of 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT HBr).

Abstract: The present invention relates to compounds of (II) and an acceptable salt or hydrate thereof method of making same.

Abstract: Provided in the present invention is a novel diaroyl carbazole compound, used together with a carbazolyl oxime ester photoinitiator to show a significant synergistic initiation effect in a photoresist composition; the best sensitising effect is shown when the molar ratio of the diaroyl carbazole compound and the carbazolyl oxime ester photoinitiator is 0.1-1.4.

Abstract: A compound 1-(naphthalen-2-yloxy)-3-(piperidin-1-yl)propan-2-ol, its synthesis, and its use as an insecticidal agent.

Abstract: Disclosed herein is a tricyclic octacationic cyclophane and complexes comprising the tricyclic octacationic cyclophane and a perylene diimide dye complexed therein and methods of using and making the cyclophane and complexes.

Abstract: Disclosed are compounds having the formula (I): wherein R1 represents a group: —NH2, —NHCORa, —NHCOORb, —(C2-C6)alkenylene-CO—NH—OH, —(C2-C6)alkynylene-CO—NH—OH or —OH; R2 represents a group: —OCH3, —OCH2CH3, —SCH3, —SCH2CH3 or —OCHF2; R3 represents a hydrogen atom or a group: —CH3, —CN, —F, —Cl or —ORc; R4 represents a hydrogen atom or a group: —CH3, —CN, —F, —Cl or —ORd; Ra represents a group: —(C1-C5)alkyl or —CF3; Rb represents a group: —(C1-C5)alkyl or —CF3; Rc represents a group: —(C1-C5)alkyl or —CF3; and Rd represents a group: —(C1-C5)alkyl or —CF3; in the state of a base or acid or acid salts or base salts or in the form of hydrate or of solvate. Also disclosed are drug conjugates including such compounds.

Abstract: A 2-(1H-imidazole-1-carbonyl)benzoic acid compound, its synthesis, and its use as an anticancer agent.

Abstract: An 3-(4,5-bis(4-bromophenyl)-2-(4-chlorophenyl)-1H-imidazol-1-yl)propanoic acid compound, its synthesis, and its use as an antimicrobial agent.

Abstract: A 4-[4,4-bis(4-chlorophenyl)-2,5-dioxoimidazolidin-1-yl]butanoic acid compound, its synthesis, and its use as an antimicrobial agent.

Abstract: The present invention is related to deuterated secnidazole, a prodrug thereof, a hydrate thereof, a solvate thereof, a polymorph thereof, or a pharmaceutically acceptable salt thereof and its use for the treatment of bacterial vaginosis or trichomoniasis in a subject in need thereof. The present invention is also related to pharmaceutical compositions and methods and uses of treating bacterial vaginosis, trichomoniasis, amoebiasis, giardiasis, or a combination thereof.

Abstract: An 2-(5-(3-fluorophenyl)-4-phenyl-4H-1,2,4-triazol-3-ylthio)acetic acid compound, its synthesis, and its use as an antimicrobial agent.

Abstract: A N?-(2-naphthoyloxy)-2-(benzo[d]oxazol-2-yl)acetimidamide compound, its synthesis, and its use as an antimicrobial agent.

Abstract: A 3-(3-bromophenyl)-5-((2-isopropyl-5-methylphenoxy)methyl)-1.2.4-oxadiazole compound, its synthesis, and its use as an antimicrobial agent.

Abstract: Novel arylhydrazones derivatives, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The arylhydrazones derivative compounds are useful as anti-tubercular agents.

Abstract: Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process.

Abstract: Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, (I) are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.

Abstract: Provided are delocalized lipophilic cation (DLC) compounds and methods of using such compounds. Also provided are pharmaceutical compositions that include a DLC compound. Provided methods include methods of killing cells and methods of fluorescently labeling mitochondria by contacting the cells with a DLC compound of the present disclosure. Also provided are methods of imaging cell mitochondria, methods of determining whether a patient has a mitochondria related disease, and methods of treating a patient for a mitochondria related disease. Kits that include compounds of the present disclosure are also provided.

Abstract: The present invention relates to a new intermediate, (2,2-dimethyl-N-[6-(1-methyl-piperidin-4-carbonyl)-pyridin-2-yl]-propanamide) useful in the synthesis of lasmiditan, to a method for obtaining same, to the use of said intermediate for preparing lasmiditan, to a method for preparing lasmiditan making use of said intermediate, and to a method for preparing an intermediate ((6-amino-pyridin-2-yl)-(1-methyl-piperidin-4-yl)-methanone) from (2,2-dimethyl-N-[6-(1-methyl-piperidin-4-carbonyl)-pyridin-2-yl]-propanamide).

Abstract: The present invention provides a compound having an excellent control effect against harmful arthropods, which is represented by formula (I) [wherein A1 represents CR1b etc., A2 represents CR1c etc., T represents a C1-C10 chain hydrocarbon group which is substituted with one or more halogen atoms etc., Q represents an oxygen atom etc., R1a, R1b and R1c are identical to or different from each other, and each represents a C1-C6 alkyl group etc., R2 represents a C1-C6 alkyl group etc., R3 represents a C1-C6 chain hydrocarbon group etc., n is 0, 1 or 2, and q is 0, 1, 2 or 3.], as well as a composition for controlling harmful arthropod comprising the same compound, and a method for controlling harmful arthropod comprising applying the same compound.

Abstract: It is provided a process for the preparation of aripiprazole lauroxil that comprises reacting 1-(hydroxymethyl) aripiprazole with lauric acid in the presence of a suitable solvent and a carboxyl activating agent in the presence of a suitable solvent and, optionally, in the presence of an appropriate base. 1-(Hydroxymethyl) aripiprazole can be prepared by reacting aripiprazol or an hydrate thereof with paraformaldehyde in the presence of a suitable organic solvent and a suitable base, wherein the reaction is carried out without the addition of water as a solvent to the reaction mixture. Additionally, (7-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butoxy)-3,4-dihydro-2-oxoquinolin-1(2H)-yl)methyl formate is provided as a reference standard.

Abstract: The present invention relates compounds of Formula (A) as H3R antagonists, as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses as modulators of Histamine 3 Receptor (H3R) functions. The present invention also relates to the uses of the compounds or pharmaceutical compositions in treating or preventing certain disorders and diseases which relate to H3R functions in humans.

Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end at least one of a Von Hippel-Lindau ligand, a cereblon ligand, Inhibitors of Apoptosis Proteins ligand, mouse double-minute homolog 2 ligand, or a combination thereof, which binds to the respective E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

Abstract: Provided herein are methods of synthesizing quinazoline compounds comprising at least one atropisomeric center.

Abstract: The present disclosure provides a compound represented by structural formula (I): or a pharmaceutically acceptable salt thereof useful for treating a cancer.

Abstract: The present disclosure relates to compounds of formula (I) and pharmaceutical compositions and their use in reducing Widely Interspaced Zinc Finger Motifs (WIZ) expression levels, or inducing fetal hemoglobin (HbF) expression, and in the treatment of inherited blood disorders (e.g., hemoglobinopathies, e.g., beta-hemoglobinopathies), such as sickle cell disease and beta-thalassemia.

Abstract: A 6-(6-bromo-2-oxo-2H-chromen-3-yl)-4-(3-bromophenyl)-2-alkoxynicotinonitrile compound, its synthesis, and its use as an antimicrobial agent.

Abstract: Linker-drug compounds and antibody-drug conjugates that bind to human oncology targets are disclosed. The linker-drug compounds and antibody-drug conjugates comprise a splicing modulator drug moiety. The disclosure further relates to methods and compositions for use in the treatment of neoplastic disorders by administering the antibody-drug conjugates provided herein. In an embodiment, the splicing modulator comprises a pladienolide or a pladienolide derivative.

Abstract: The present invention relates to a medicament for treating or preventing central nervous system disease whose cause is related to abnormal aggregation of proteins in the brain, which comprises as an active ingredient a compound of formula (1) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are hydrogen, etc., R3 and R4 are hydrogen, C1-6 alkyl, etc., R5 is halogen, C1-6 alkyl, etc., R6 is hydrogen, halogen, etc., X is oxygen, etc., Y is carbon, etc., m and n are an integer of 0, 1, etc., r and s are 0, 1, 2, etc., Hy is pyridine ring, etc., which has an action of suppressing or reducing the accumulation of abnormal aggregation of proteins in the brain.

Abstract: Provided herein, inter alia, are splice modulator compounds. The compounds include optically pure, stereospecific analogs of FD-895. The methods provided herein allow, for example, for scalable preparation of said compounds, and further allow, for example, use of said compounds for inhibiting spliceosome activity.

Abstract: Disclosed is a histone acetyltransferase (HAT) inhibitor. Provided are a compound represented by the general formula I, a pharmaceutically acceptable salt, a stereoisomer, an enantiomer, a diastereoisomer, an atropisomer, a racemate, a polymorph, a solvate or an isotope-labeled compound (including deuterium substitution) thereof, a preparation method therefor, a pharmaceutical composition comprising same and use thereof in the treatment of various HAT-related diseases or conditions.

Abstract: Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1.

Abstract: The invention described herein relates to the compounds of Formula I for treating diseases and disorders for which inhibition or modulation of the topoisomerase I enzyme produces a physiologically beneficial response, in particular for the treatment of breast cancer. Also provided is the process of preparing compounds of Formula I.

Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R3, R4A, R4b, and R5, are as defined herein, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of CLL.

Abstract: The invention relates to kinase inhibitors, in particular inhibitors of protein kinases including the protein-tyrosine kinases LCK, ABL, SRC, KIT, SIK-family and/or their mutants. Although structurally similar to dasatinib, the kinase inhibitors of the invention can display one or more certain properties distinct to dasatinib. Also, the invention relates to pharmaceutical compositions that comprise one or more of the kinase inhibitors. The kinase inhibitors or pharmaceutical compositions of the invention may be used in the treatment of a disorder or condition, such as a proliferative disorder, for example, a leukaemia or solid tumour. The kinase inhibitors or pharmaceutical compositions may be used in a treatment regimen that corresponds to, is similar to or is distinct from that used with dasatinib for a corresponding disorder, and in particular may be used in a combination treatment regimen together with one or more additional therapeutic agents, such as immune-checkpoint inhibitors.

Abstract: The invention provides a compound of formula (I): or a pharmaceutically-acceptable salt thereof, that is an inhibitor of JAK kinases. The invention also provides pharmaceutical compositions comprising such compound, a crystalline form, methods of using such compound to treat inflammatory skin diseases and other diseases, and processes and intermediates useful for preparing such compound.

Abstract: Disclosed are compounds of Formula (I) N-oxides, or salts thereof, wherein X is CR1 or N; and G, A, R1; and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

Abstract: The present invention relates to methyl {4,6-diamino-2-[5-fluoro-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate in the form of a novel active compound product having improved properties, for example in respect of the isolability of the active compound product, the dischargeability of the active compound product after isolation and drying and also conveyability, sieveability and micronizability of the active compound product, and to processes for the production and formulation thereof.

Abstract: Substituted Pyrazolo-pyridines as GluN2B receptor ligands. Such compounds may be used in GluN2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by GluN2B receptor activity.

Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.

Abstract: The present invention relates to solid forms of the insecticide of formula (I): compositions comprising the solid forms and methods of their use as insecticides.

Abstract: Provided herein are, inter alia, methods of treating cancer using compounds of the invention.

Abstract: Novel pyrido[3,4-e][1,2,4]triazolo[4,3-c]pyrimidine compounds, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The pyrido[3,4-e][1,2,4]triazolo[4,3-c]pyrimidine compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.

Abstract: Compounds that inhibit Protein Arginine N-Methyl Transferase 5(PRMT5) activity, as well as method for their preparation and use are provided. Specifically, compounds of Formula (I) and pharmaceutically acceptable salts, hydrates and solvates, as well as method for their preparation and use are provided.

Abstract: Novel pyrrolo[3,2-c][2,6]naphthyridine-2-carboxylic acid compounds, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The pyrrolo[3,2-c][2,6]naphthyridine-2-carboxylic acid compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.