Abstract: The present disclosure provides treprostinil derivatives that can act as prodrugs of treprostinil. The treprostinil derivatives can be used to treat any conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension.

Abstract: A process for converting caprolactam to aminocapronitrile, the process comprising contacting a caprolactam feed with ammonia and an aluminosilicate zeolite catalyst to produce an aminocapronitrile product, wherein the catalyst comprises less than 5 wt. % of an active metal, and wherein conversion is greater than 50% and selectivity for aminocapronitrile is greater than 91%.

Abstract: The invention provides a method for the extraction of an organic acid (10) from a mixture (110), the method comprising: an extraction stage comprising providing the mixture (110) to a sorbent (150); an elution stage comprising passing an eluent along the sorbent (120) to provide an eluate (140), wherein the eluent (130) comprises a solvent selected from the group consisting of acetone and alcohols, and wherein the eluent (130) comprises at least 0.1 M of OH—, and wherein the eluent (130) comprises at least 0.1 M of an cation selected from the group comprising Na+, K+, Ca2+, Mg2+ and NH4+; a precipitation stage comprising providing CO2 (150) to the eluate (140), wherein the CO2 (150) and the cation form a carbonate, wherein the carbonate precipitates; and a separation stage comprising separating the organic acid (10) from the eluate (140).

Abstract: The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.

Abstract: An object of present invention is to provide a compound or a salt thereof constituting lipid particles that can achieve a high nucleic acid encapsulation rate and excellent delivery of nucleic acids, and to provide lipid particles and pharmaceutical composition using the compound or a salt thereof, which can achieve a high nucleic acid encapsulation rate and excellent delivery of nucleic acids. According to an aspect of the present invention, a compound represented by Formula (1) or a salt thereof is provided. In the formula, each symbol has a meaning defined in the present specification.

Abstract: Disclosed are benzoate derivatives. Provided is a compound having a formula selected from the group consisting of following structures. The compound can be used for quality control over a 2-(diethylamino)ethyl 2-acetoxybenzoate hydrochloride product, and also for inflammation diminishment.

Abstract: This application relates to solabegron zwitterion useful for the treatment of lower urinary tract symptoms such as, for example, overactive bladder and prostate disorders. Additionally, this application relates to pharmaceutical compositions and methods of treatment utilizing the solabegron zwitterion for treating lower urinary tract symptoms. This application also relates to methods of preparing solabegron hydrochloride from the solabegron zwitterion.

Abstract: The present invention provides a compound having the structure: and use of the compound for inhibiting the growth of or killing

Abstract: Disclosed is a process for the preparation of Omaveloxolone and salts thereof, as well as intermediates thereof.

Abstract: Provided herein are compounds and compositions thereof for modulating S1P5. In some embodiments, the compounds and compositions are provided for treatment of neurological diseases.

Abstract: Inhibitors of SARS-COV-2 (COVID), pharmaceutical compositions comprising same; and methods of treating a severe acute respiratory syndrome.

Abstract: The present invention relates to an amino lipid compound, namely a compound represented by chemical formula I, or a stereoisomer, tautomer, pharmaceutically acceptable salt, or prodrug thereof. Moreover, also disclosed are a preparation method for the compound and the use of the compound in delivering a genetic material and preparing a drug.

Abstract: Hallucinogenic and non-hallucinogenic serotonin receptor agonists are disclosed herein in addition to methods of making and using the same.

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 novel indole derivative and a use thereof. The novel indole derivative according to the present invention traps methylglyoxal (MGO), which is a main precursor of advanced glycation end products, and thus can be effectively used for preventing, improving, or treating diseases related to advanced glycation end products.

Abstract: LpxH targeting compounds, compositions thereof, as well as methods for for making and using the same are disclosed herein. The LpxH target compounds typically have a structure pursuant to Formula (I) and/or a salt thereof, wherein Rb is selected from a single bond, C4 to C10 unsubstituted aryl, C4 to C10 substituted aryl, unsubstituted or substituted four to ten member heterocycle ring, C1 to C10 unsubstituted alkyl, and C1 to C10 substituted alkyl; Rc comprises hydrogen, halogen, —OH, —CO2CH3, —COOH, —CN2CF3, —CF3, —C2OH, —CONHOH, —CCOH, C4 to C10 unsubstituted aryl, C4 to C10 substituted aryl, unsubstituted or substituted four to ten member heterocycle ring, C1 to C10 unsubstituted alkyl, or C1 to C10 substituted alkyl; and Rd and Re are independently hydrogen, —OH, —COH, —COH, —COC, —COOH, Rf, or are taken together as an unsubstituted or substituted four to eight member nitrogen containing heterocycle ring.

Abstract: A first aspect of the present invention provides a method for the preparation of 2-chloro-5-chloromethylpyridine, comprising: performing a cyclization reaction on 4,5-dichloro-4-methoxypentanenitrile in presence of a silicon compound and an acylamide compound to obtain 2-chloro-5-chloromethylpyridine. Another aspect of the present invention provides a method for preparation of 2-(chloromethyl)-5-(trifluoromethyl)-1,3,4-oxadiazole, comprising: performing a cyclization reaction on 1-(chloroacetyl)-2-(trifluoroacetyl)hydrazine in a presence of a silicon compound and an acylamide compound to obtain 2-(chloromethyl)-5-(trifluoromethyl)-1,3,4-oxadiazole. The silicon compound or/and acylamide compound provided by the present invention serve as cyclization reagents and have high efficiency.

Abstract: The application describes methods for making a deuterated dextromethorphan of Formula (I), deuterated dextromethorphan produced by these methods, and pharmaceutically acceptable salts thereof.

Abstract: A system includes at least one processor, a message system running on the at least one processor to create an actionable widget card, the message system includes a database to store parameters for the actionable widget card and pre-defined rules concerning card definitions; and at least one card product system to receive a trigger and to generate the actionable widget card according to said trigger, where the message system enables communication via the actionable widget card between a backend non-interactive external system and at least one user of the backend non-interactive external system.

Abstract: The present invention relates to a composition for preventing, improving, or treating diseases related to advanced glycation end products, comprising an indole derivative or a pharmaceutically acceptable salt thereof. Specifically, the composition of the present invention possesses the effect of trapping methylglyoxal (MGO), which is a main precursor of advanced glycation end products, and thus can be effectively used for preventing, improving, or treating diseases related to advanced glycation end products.

Abstract: The present invention relates to novel lignin-derived compounds and compositions comprising the same and their use as redox flow battery electrolytes. The invention further provides a method for preparing said compounds and compositions as well as a redox flow battery comprising said compounds and compositions. Additionally, an assembly for carrying out the inventive method is provided.

Abstract: Provided herein are compounds of Formula (I?), Formula (I?), Formula (I), Formula (II?), and Formula (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. Also provided are methods, uses, and kits involving the disclosed compounds and pharmaceutical compositions thereof for treating and/or preventing diseases (e.g., proliferative diseases (e.g., cancers), inflammatory diseases (e.g., fibrosis), autoimmune diseases (e.g., sclerosis)) in a subject. Provided are methods of inhibiting the activity of a transcription factor (e.g., TEAD, such as TEAD1, TEAD2, TEAD3, TEAD4) and/or inhibiting the transcription of a gene (e.g., a gene controlled or regulated by a transcription factor (e.g., TEAD)) in a subject.

Abstract: A compound represented by the following general formula (B1). Further disclosed is a corrosion inhibitor (B) containing one or more selected from the compound represented by the following formula (B1). Further disclosed is a lubricant composition containing an ionic liquid (A) and the corrosion inhibitor (B). The compound and the corrosion inhibitor are excellent in stability in any of a high vacuum, a low-temperature environment, a high-temperature environment, and an ordinary temperature-ordinary pressure environment, and the lubricant composition containing the corrosion inhibitor is excellent in metal corrosion resistance, solubility, and low evaporability. In the general formula (B1), M is an alkali metal and RB11 is an alkylene group having 1 to 19 carbon atoms.

Abstract: Compounds of formula (1): wherein R1 represents a —C(R2)(R3)—[C(R4)(R5)]m-L-R6 group or —R7; and the preparation and the therapeutic uses of the compounds of formula (1) as agonists of TRPM8 receptors, useful especially in the treatment of oropharyngeal dysphagia.

Abstract: The present application discloses a class of guaianolide sesquiterpene lactone derivatives and pharmaceutical use thereof. The guaianolide sesquiterpene lactone derivative or a pharmaceutically acceptable salt thereof is shown as general formula I. In the present application, a class of novel guaianolide sesquiterpene lactone derivatives are found by structural optimization with abundant natural ingredients such as parthenolide and dehydrocostus lactone as raw materials, which derivatives have good inhibitory activity on the activation of the NLRP3 inflammasome, and the chemical stability, water solubility and oral bioavailability of which are significantly improved, and it is verified by experiments that the derivatives have inhibitory effects on the activity of the NLRP3 inflammasome and have potential pharmaceutical applications.

Abstract: Small molecule inhibitors that block the interaction between B-cell lymphoma 10 protein (BCL10) and mucosa- associated lymphoid tissue lymphoma translocation protein 1 (MALT1), thereby inhibiting both the protease and scaffolding activities of MALT1, and MALT1- dependent downstream signaling, including IL-6 and IL-10 secretion by B-cell lymphoma cells and IL-2 transcription and secretion by Jurkat T cells.

Abstract: Provided are deuterated analogs of MDMA, including deuterated empathogens. In some embodiments, such compounds are monoamine releasers or inhibit monoamine transporters. In some aspects, features of the compounds provide stability, such as metabolic stability, and efficacy. Also provided are methods for the preparation of deuterated empathogens and pharmaceutical compositions comprising the same. Methods of using the deuterated empathogens, alone or in combination with other therapeutic agents, are provided. In some embodiments, deuterated empathogens are used to treat CNS disorders, such as mental health conditions and neurodegenerative disorders.

Abstract: The present disclosure relates generally to compounds that bind to and act as degraders of an IKAROS Family Zinc Finger (IKZF) protein, such as IKZF2 (Helios) and/or IKZF4 (Eos). The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding and degradation of an IKZF protein, such as IKZF2 and/or IKZF4, including cancer.

Abstract: Provided herein is a compound of formula (XXXII) or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer thereof or a physiologically functional derivative thereof, wherein R1, R2, R3, G, A, E, n, p, and q are defined herein. Also provided herein are compositions comprising a compound of formula (XXXII), and methods of using a compound of formula (XXXII), e.g., in the treatment or prevention of skin disorders.

Abstract: Methods are provided for modulating MRGPRX2 generally, or for treating a MRGPRX2 or a MRGPRX2 ortholog dependent condition, more specifically, by contacting the MRGPRX2 or the MRGPRX2 ortholog by administering to a subject in need thereof, respectively, an effective amount of a compound having structure (I): or a pharmaceutically acceptable salt, isomer, hydrate, solvate or isotope thereof, wherein W, Z, R1, R2, R3, R4, R5, R6 and Rx are as defined herein. Pharmaceutical compositions containing such compounds, as well as the compounds themselves, are also provided.

Abstract: Methods are provided for modulating MRGPRX2 generally, or for treating a MRGPRX2 or a MRGPRX2 ortholog dependent condition, more specifically, by contacting the MRGPRX2 or the MRGPRX2 ortholog by administering to a subject in need thereof, respectively, an effective amount of a compound having structure (I): or a pharmaceutically acceptable salt, isomer, hydrate, solvate or isotope thereof, wherein W, Z, R1, R2, R3, R4, R5, R6 and Rx are as defined herein. Pharmaceutical compositions containing such compounds, as well as the compounds themselves, are also provided.

Abstract: Methods are provided for modulating MRGPRX2 generally, or for treating a MRGPRX2 or a MRGPRX2 ortholog dependent condition, more specifically, by contacting the MRGPRX2 or the MRGPRX2 ortholog by administering to a subject in need thereof, respectively, an effective amount of a compound having structure (I): or a pharmaceutically acceptable salt, isomer, hydrate, solvate or isotope thereof, wherein W, Z, R1, R2, R3, R4, R5, R6 and Rx are as defined herein. Pharmaceutical compositions containing such compounds, as well as the compounds themselves, are also provided.

Abstract: The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.

Abstract: Provided herein are phosphodiesterase 4 (PDE4) degraders, e.g., a compound of Formula (I) or (IA), and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a PDE4-mediated disease, disorder, or condition.

Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules as defined within Formula I (as defined herein) which function as inhibitors of glucose-regulated protein 78 (GRP78) within cancer cells and/or immune cells, and which function as effective therapeutic agents for treating, ameliorating, and preventing various forms of cancer (e.g., pancreatic cancer), viral infections (e.g. SARS-CoV-2), and inflammatory diseases. In addition, this invention also relates to a new class of PROTACs having Formulas II, III and IV (as defined herein) which function as degraders of GRP78 within cancer and/or immune cells. Pharmaceutical compositions comprising said compounds of Formulas I, II, III, or IV are also within the scope of the present invention.

Abstract: The present disclosure provides novel compounds and their metal chelates, for diagnostic, therapeutic and/or theranostic use in the treatment of cancer, tumor and other oxygen activity related diseases. The novel compounds are analogues of bleomycin (BLM).

Abstract: There are disclosed compounds of the following formula I: or a stereoisomer or pharmaceutically acceptable salt thereof, wherein all substituents are as defined herein, which are useful in the modulation of IL-12, IL-23 and/or IFN?, by acting on Tyk-2 to cause signal transduction inhibition. The compounds of the invention may be useful for treating neurodegenerative diseases or disorders.

Abstract: The disclosure is directed to compounds of Formula I Pharmaceutical compositions comprising compounds of Formula I, as well as methods of their use and preparation, are also described.

Abstract: Pyrimidine and Pyridine containing compounds are described herein that are enzyme p70S6K inhibitors useful in the treatment of S6K-dependent or S6K-mediated diseases and conditions, including but not limited to cancer, fibrotic metabolic and certain neurological disorders.

Abstract: The present invention relates to solid forms of (5S)-cyclopropyl-5-[3-[(3S)-4-(3,5-difluorophenyl)-3-methyl-piperazin-1-yl]-3 -oxo-propyl]imidazolidine-2,4-dione and to pharmaceutical preparations comprising them and methods of their manufacture, as well as the use of said solid forms or preparations for the prophylaxis and/or treatment of inflammatory conditions, muscular disease, fibrotic diseases, viral infection, and/or diseases involving degradation of cartilage and/or disruption of cartilage homeostasis, especially osteoarthritis.

Abstract: The present disclosure encompasses solid state forms of Belumosudil, in embodiments crystalline polymorphs of Belumosudil or salts thereof, processes for preparation thereof, and pharmaceutical compositions thereof.

Abstract: Disclosed herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, that are inhibitors of Polo Like Kinase 4 (PLK4). Also disclosed herein are pharmaceutical compositions comprising the compounds of Formula (I), or pharmaceutically acceptable salts thereof, and one or more pharmaceutically acceptable excipients. Further disclosed herein are methods of treating cancer in a subject in need thereof, comprising administering to the subject an amount of a compound of Formula (I), or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to compounds of Formula (I) wherein X, Ar1, Ar2, L, n, m, and R1 are as described in the description, their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of Formula (I), and especially to their use as Galectin-3 inhibitors.

Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, PCSK9, or a pharmaceutically acceptable salt, solvate, prodrug or polymorph thereof, and to compositions and formulations comprising such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I): (I) wherein R1, R2, R3 and L are described herein.

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: Although compounds for treating or ameliorating malignant diseases have been proposed, patients had to endure a large burden since many of such compounds could not be orally ingested. Mangiferin has an effect of ameliorating malignant diseases through oral ingestion. However, such effect is minor and realistically it was not easy to ingest mangiferin. Further, in order to develop more effective pharmaceutical agents and the like for treating malignant diseases, it has been considered constantly necessary to obtain new or improved forms of an existing medical agent for inhibiting kinases such as NIK. Compounds represented by formula (1), formula (2), formula (3), formula (4), formula (5), formula (6), formula (7), formula (8), formula (9), formula (10), formula (11), and formula (12) have an effect of ameliorating malignant diseases through oral ingestion, and can exhibit said effect with an amount less than that for mangiferin.

Abstract: The present invention relates to compounds of formula (I), wherein A is a 3-10 membered carbocyclyl or a 4-12 membered heterocyclyl containing 1-4 heteroatoms selected from O, N, or S; B is any of the following groups (1), (2), or (3); C is any of the following groups (1?), (2?), (3?), or (4?); G1 is CH2, NH, or O; G2 and G3 are, independently, CH or N; Z is —C(O)—, —SO2—, —C1-3 alkyl-, or —CH2—C(O)—; L is a bond, —C1-7 alkyl-, or —C1-7 alkenyl-. The compounds of formula (I) are cytochrome P450 monooxygenase 11A1 (CYP11A1) inhibitors. The compounds are useful as medicaments in the treatment of steroid receptor, for example, androgen receptor or estrogen receptor, dependent diseases and conditions, such as cancer including prostate cancer and estrogen cancer.

Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as a pesticides, especially as herbicides.

Abstract: The present invention relates to an organic compound and an organic light-emitting device comprising same, the organic compound being employed in an organic layer, such as an electron-transporting layer, in an organic light-emitting device and in a luminous efficiency-improving layer (a capping layer) provided in an organic light-emitting device to achieve light-emitting characteristics such as superior luminous efficiency and low-voltage driving of a device. The present invention can realize improved device characteristics such as superior luminous efficiency and low-voltage driving and thus can be industrially usefully employed in various lighting and display devices.

Abstract: Compounds as inhibitors of Activating Transcription Factor 6 (ATF6) are provided. The compounds may find use as therapeutic agents for the treatment of diseases or disorders mediated by ATF6 and may find particular use in the treatment of viral infections, neurodegenerative diseases, vascular diseases, or cancer.