Abstract: The present invention relates to a method for preparing a dicarboxyl acid aromatic heterocyclic compound and a dicarboxyl acid aromatic heterocyclic compound obtained thereby. According to the present invention, an oxide with improved yield and purity can be produced by an oxidation reaction of a bio-based hydroxyl-free aromatic heterocyclic compound under a heterogeneous catalyst.

Abstract: A method for asymmetric synthesis of (?)-Anisomelic Acid is provided in the present invention, a chiral compound (?)-Costunolide is used as a starting material, a key intermediate is obtained by a regioselective ozone decomposition reaction, then carbon chain extension is performed by a Horner-Wadsworth-Emmons (HWE) reaction and a Peterson olefination reaction, and a (?)-anisomelic acid fourteen-membered carbocyclic skeleton is constructed by a ring-closing metathesis (RCM) reaction, laying an important foundation for subsequent (?)-anisomelic acid biological activity research, in the synthesis route, various (?)-anisomelic acid analogs can also be obtained from the key intermediate, the reaction operations in the synthesis route are simple and the present invention can be widely popularized and used.

Abstract: A biflavone compound against an I-type herpes simplex virus, and a preparation method therefor and the use thereof. The bioflavone compound is a compound of formula I, or a crystal form thereof, or a salt thereof, or a stereoisomer thereof, or a solvate thereof, or a hydrate thereof, or a prodrug thereof. The biflavone compound has a good inhibitory effect on the I-type herpes simplex virus, has a significant effect on the replication and direct inactivation of the virus, and is dose dependent. The compound is also effective in preventing and/or treating viral keratitis caused by the I-type herpes simplex virus. The compound has good water solubility and low toxicity. It can be prepared into an external preparation for resisting the I-type herpes simplex virus, such as eye drops and eye ointment, and external ointments, creams, gel agents, film agents, film-coating agents, etc.

Abstract: Provided herein is a method for producing an ionizable lipid that comprises: (i) reacting fatty esters in a Claisen condensation reaction in the presence of a catalyst, the Claisen condensation employing a weak base and carried out at a temperature of between ?10 and 60 degrees Celsius to produce a ketoester; (ii) reacting the ketoester produced in step (i) under conditions to produce a ketone from the ketoester in one or more steps via a hydrolysis and decarboxylation of the ketoester; and (iii) preparing the ionizable lipid from the ketone thereof using one or more synthesis steps resulting in an addition of an ionizable head group moiety to (a) the ketone; or (b) an alcohol produced from an optional reduction of the ketone to produce the alcohol, thereby producing the ionizable lipid. The ionizable lipid produced in step (iii) may be formulated in a drug delivery vehicle.

Abstract: Provided are fluorinated analogs of MDMA, including fluorinated 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 fluorinated empathogens and pharmaceutical compositions comprising the same. Methods of using the fluorinated empathogens, alone or in combination with other therapeutic agents, are provided. In some embodiments, fluorinated empathogens are used to treat CNS disorders, such as mental health conditions and neurodegenerative disorders.

Abstract: This invention provides a method for synthesizing glycolide using methyl glycolate as a raw material, comprising two steps as illustrated in the following reaction formulas: wherein, the ROH represents a straight/branched chain alcohol, acid or ester containing 18-30 carbons and at least one hydroxyl group. The method for glycolide synthesis disclosed in the present invention manages to maintain a low viscosity within the reaction system by introducing a high-boiling alcohol into the reaction system to form a larger alkoxy glycolate exhibiting a significantly lower molecular weight compared to the typical glycolic acid oligomers utilized in the conventional process. Thus the challenges of coking and inefficient heat transfer encountered in traditional glycolide synthesis routes are effectively addressed.

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: The present invention provides a compound of formula (I): wherein R1, R2, R3, R4, k, l, m and n are as defined in the specification, or a pharmaceutically acceptable salt thereof with the effect of inhibiting T-type calcium channels and a medicament useful for the treatment of a disease associated with the activation of T-type calcium channels.

Abstract: There is provided herein a compound of formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, X1, X2, Y1 to Y4, Z1 to Z3, and n have meanings provided in the description.

Abstract: Provided are a quaternary ammonium salt compound, a preparation method therefor and a use thereof. The compound represented by general formula (I), or an isomer or pharmaceutically acceptable salt thereof, and a composition thereof can be used for the preparation of anesthetic or analgesic drugs. Each substituent of general formula (I) is the same as in the definition of the description.

Abstract: Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof wherein A, E, U, X, Y, Z, R1, R2 and n are as defined herein. The compounds of Formula I act as IL4I1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for IL4I1-related diseases. Also provided herein are pharmaceutical compositions comprising the compounds of the invention, or their pharmaceutically acceptable salts, and a pharmaceutically acceptable carrier and methods of treatment with the compounds of the invention.

Abstract: The present invention relates to macrocyclic compounds of any one of Formula (I), or a pharmaceutically acceptable form thereof, pharmaceutical compositions comprising the same, methods of preparing the same, and methods of treating cancer dependent on a farnesylated protein, using the same.

Abstract: BA-1049 (R) and its active metabolite are disclosed. Also disclosed are pharmaceutical formulations containing BA-1049 (R) or its active metabolite.

Abstract: The present invention relates to new tetrahydroquinoline (THQ) compounds and new methods for synthetizing such compounds. The present invention relates to the applications thereof, in particular in therapeutic treatment. The present invention relates in particular to compound having the following structure: wherein R, R?, RA, Nu, R1, R2, R3, and R4 are each independently an atom or a chemical group of atoms.

Abstract: A substituted triazinylmethylcycloalkylcarboxylic acid derivative having a structure as shown in formula (I). In addition, further disclosed are a pharmaceutically acceptable salt, a stereoisomer, a pharmaceutical composition and the use of the derivative. The compound has significant P2X3 inhibitory activity and selectivity, and is high in application value.

Abstract: An efficient and economical method for synthesizing Fasudil hydrochloride includes the synthesis route starts with inexpensive and readily available ethylenediamine as the starting material, obtains intermediate tert butyl-(N-(2-aminoethyl)-5-isoquinoline sulfonamide) carbamate (5) through sulfonylation and Boc protection, and then obtains Fasudil hydrochloride through a stacking process, which includes four steps: nucleophilic substitution, deprotection, cyclization, and salt formation. The total yield of Fasudil hydrochloride (1) is 67.1%, with a purity of up to 99.94%. Compared with traditional processes, the route avoids the use of expensive homopiperazine and its derivatives as synthetic intermediates. The advantages of the process include cheap and easy to obtain raw materials, simple operation, low cost, environmental friendliness, and suitability for industrial production.

Abstract: The present invention relates to phenyluracils of formula (I) or their agriculturally acceptable salts or derivatives, wherein the variables are defined according to the description, compositions comprising them and their use as herbicides. i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidal effective amount of at least one phenyluracil of formula (I) to act on plants, their seed and/or their habitat.

Abstract: The present disclosure discloses sulfonamides, methods for preparation thereof and uses thereof, belonging to the technical field of medicinal chemistry. The structure of the sulfonamides of the present disclosure is shown in Formula I. The present disclosure also provides use of the compound of Formula I or a salt, solvate, isomer, metabolite, nitrogen-oxide, or prodrug thereof in the manufacture of a medicament for the treatment or prevention of P2X3 and/or P2X2/3 receptor-associated diseases. The sulfonamides of the present disclosure have a potent cough suppressing effect and a significantly prolonged action. Their inhibitory activity against P2X3 is superior to that of Comparative compound 1 and the positive control Gefapixant.

Abstract: The invention relates to substituted 6-substituted isoquinoline oxide compounds of formula (V) and to a process for making them. The compounds of formula (V) can be used as intermediates for making 6-substituted-1-(2H)-isoquinolinone compounds of formula (I) The compounds of formula (I) are inhibitors of the enzyme Rho-kinase, or can be used as intermediates in the preparation of further inhibitors of the Rho-kinase enzyme.

Abstract: The invention relates to substituted 6-substituted isoquinoline oxide compounds of formula (V) and to a process for making them. The compounds of formula (V) can be used as intermediates for making 6-substituted-1-(2H)-isoquinolinone compounds of formula (I) The compounds of formula (I) are inhibitors of the enzyme Rho-kinase, or can be used as intermediates in the preparation of further inhibitors of the Rho-kinase enzyme.

Abstract: The present invention relates to a novel quinoline or quinazoline compound and the use thereof. The compound according to the present invention shows an excellent inhibitory activity against cytochrome P450 4A (CYP4A) and thus may be utilized for preventing, relieving or treating metabolic diseases.

Abstract: Disclosed herein is a compound, or a pharmaceutically acceptable salt thereof, that has a formula MTG2-L-ME3. MTG2 is a moiety that binds to tissue transglutaminase 2 (TG2), L is a bond or a linker covalently attaching MTG2 and ME3, and ME3 is a moiety that binds to an E3 ubiquitin ligase. Disclosed herein are also the uses of the compound, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same, in a method of treating a disease or disorder associated with TG2 activity or in a method of inhibiting cell proliferation.

Abstract: Provided herein are substituted indole compounds. In certain embodiments, the compounds are inhibitors of the alternative pathway of the complement system, and in particular, inhibitors of complement factor B (CFB). Also provided are compositions comprising the compounds and methods of use thereof. The compounds provided are useful in the treatment, prevention or amelioration of a disease, condition or disorder through inhibition of the complement alternative pathway.

Abstract: The invention provides a novel synthetic route for the preparation of the Chk-1 inhibitor compound: as well as novel process intermediates per se.

Abstract: The present disclosure relates to compounds suitable for the inhibition of protein arginine methyl-transferase (PRMT), in particular PRMT5. These compounds may be for use as therapeutic agents, in particular, agents for use in the treatment and/or prevention of proliferative diseases, such as cancer.

Abstract: Disclosed are compounds and salts thereof that bind to and modulate cereblon activity. In some embodiments, the binding and modulation of cereblon results in the degradation of IKAROS family zinc finger proteins (e.g., IKZF2). The compounds are of formula (I): (I).

Abstract: A quinoxaline compound and application thereof are described. In an example, the quinoxaline compound has a high glass transition temperature and molecular thermal stability, suitable HOMO and LUMO energy levels, and high electron mobility, and can effectively improve luminous efficiency and service life of an organic electroluminescent device after being applied to preparation of the device.

Abstract: The present disclosure relates to chemical compounds that modulate pantothenate kinase (PanK) activity for the treatment of metabolic disorders (such as diabetes mellitus type II), neurologic disorders (such as pantothenate kinase-associated neurodegeneration), pharmaceutical compositions containing such compounds, and their use in treatment. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

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

Abstract: The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.

Abstract: The present invention relates to a novel compound having inhibitory activity against pendrin, and pharmaceutical uses thereof, and provides a compound represented by formula 1 below, an E- or Z-isomer thereof, an optical isomer thereof, a precursor thereof, a pharmaceutically acceptable salt thereof, a solvate thereof or a mixture of two or more isomers thereof, and a composition for preventing, relieving or treating respiratory diseases and a diuretic composition, each composition utilizing the inhibitory activity of the compound against pendrin.

Abstract: A class of ketoamide derivatives and an application thereof are disclosed. Specifically disclosed are a compound of formula (IV) and a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to a mesylate or ethanesulfonate salt of the compound as represented by formula (I), a preparation method therefor, a pharmaceutical composition comprising the salt, and an application of the salt.

Abstract: The present invention relates to the field of chemical pharmacy, relates to a crystal form of a pyrimidine derivative and a preparation method therefor, and specifically relates to crystal forms A, B, C, D, and E of a compound of formula (I), a preparation method therefor, and a pharmaceutical composition and use thereof. The present invention solves the problems of small granularity, poor fluidity, poor stability and the like of the compound of formula (I) present in an amorphous form. The crystal form prepared by the present invention and the pharmaceutical composition thereof can be used for preparing a drug for treating a cancer disease.

Abstract: The present application relates to a compound of Formula (I) or a pharmaceutically acceptable salt and/or solvate thereof, or a radionuclide complex comprising a compound of Formula (I) or a pharmaceutically acceptable salt and/or solvate thereof, and one or more radionuclides, and to compositions thereof. The present application also includes methods of using the compounds, complexes and compositions for targeting neurotensin receptors, and further to their use in the imaging, diagnosis and treatment of diseases, disorders or conditions such as cancer. The present application relates to a compound of Formula (II) or a pharmaceutically acceptable salt and/or solvate thereof, and to compositions and uses thereof, for example, in the treatment of diseases, disorders or conditions such as cancer.

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.

Abstract: The present invention provides acyl sulfonamide compounds of general formula (I): in which R1, R2, R3, R4, R5 and R6 are as described and defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients as well as methods of treatment and/or prophylaxis of diseases, particularly cancer, more particularly cancer in which KAT6A and/or KAT6B is focally amplified, said method comprising administering an effective amount of at least one compound of formula (I) to a subject in need thereof.

Abstract: A method of treating cancer in a subject includes administering to the subject a therapeutically effective amount of a small molecule agonist of EphA2 receptor protein, the small molecule having a general formula: A-L-X-Z (I).

Abstract: Disclosed are compounds of formula (I) wherein G1 is as antagonists of the muscarinic acetylcholine receptor M4 (mAChR M4) for use in the treatment of e.g. a neurodegenerative disorder, a movement disorder, or a brain disorder, such as e.g. Parkinson's disease, drug-induced Parkinsonism, dystonia, Tourette's syndrome, dyskinesias, schizophrenia, cognitive deficits associated with schizophrenia, excessive daytime sleepiness, attention deficit hyperactivity disorder (ADHD), Huntington's disease, chorea, cerebral palsy, and progressive supranuclear palsy. An exemplary compound is e.g. (2,5-difluoro-4-(6-(((3aR,5s,6aS)-2- ((tetrahydro-2H-pyran-4-yl)methyl)octahydrocyclopenta[c]pyrrol-5- yl)amino)pyridazin-3-yl)phenyl)(imino)(methyl)-?6-sulfanone (e.g. example 12; compound no. 7) Pharmacological data on the activity of the compounds in an mAChR M4 cell-based assay are provided (e.g. table 2) TABLE 2 Human M4 Cpd. No. IC50 (nM) Emin (%)* 1 13.4 4 2 39.6 2 3 18.

Abstract: The present disclosure relates generally to methods for the preparation of Compound (I).

Abstract: Provided are an oxazole derivative, a preparation method therefor, and a pharmaceutical composition comprising the same as an active ingredient for preventing or treating an allergic disease such as asthma or atopy, where the oxazole derivative exhibits an excellent inhibitory effect on the intracellular signaling of IL-33 and thus can be advantageously used as an active ingredient in a pharmaceutical composition for prevention or treatment of an allergic disease such as asthma or atopy.

Abstract: An object of the present invention is to provide a compound having an ETA receptor antagonistic effect, etc. The object can be attained by a compound represented by the following formula (1): wherein variables are as described herein, or a pharmaceutically acceptable salt thereof.

Abstract: Small molecule compounds that selectively bind to non-canonical G-quadruplex (G4) structures, such as G4s in DNA found in various types of genes described herein, along with methods of using the compounds to reduce or inhibit protein (e.g., N-Myc protein) expression in cells, such as cancer cells. The compounds have a structure according to formulas described herein, or a stereoisomer, tautomer, or pharmaceutically effective salt or ester thereof.

Abstract: The disclosure provides a compound of formula I: or a salt thereof, wherein R1, R2, R4, L1, L2, and A have any of the values described in the specification, as well as compositions comprising a compound of formula (I). The compounds are useful as TRPV4 antagonists.

Abstract: The invention relates to new 4-(piperazin-1-yl)-2-(trifluoromethyl)-1H-indoles and 4-(piperazin-1-yl)-2-(trifluoromethyl)-1H-benzimidazoles represented by formula (I), wherein all symbols and variables are as defined in the description. The compounds can find use in a method of prevention and/or treatment of diseases selected from the group consisting of Alzheimer's disease, Parkinson's disease, Levy body dementia, dementia-related psychosis, schizophrenia, delusional syndromes and other psychotic conditions related and not related to taking psychoactive substances, depression, anxiety disorders of various aetiology, sleep disorders of various aetiology.

Abstract: Disclosed herein, inter alia, are a process for the preparation of 2-bromolysergic acid diethylamide (2-Br-LSD), or a pharmaceutically acceptable salt thereof, via the controlled hydrolysis of bromocriptine to form 2-bromolysergic acid, followed by amidation to form 2-Br-LSD, the purified 2-Br-LSD, per se, and pharmaceutical compositions containing the purified 2-Br-LSD, per se, and uses thereof.

Abstract: The present disclosure relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity of PI3K-? enzymes with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with PI3K-? signaling with the compounds and compositions of the disclosure.

Abstract: Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting HPK1 activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer.

Abstract: Provided are compounds of the Formula I, and salts, hydrates and solvates thereof: wherein R1, Q, Ra, Rb, Rc, Rd and Re are each as defined in the specification. The compounds are inhibitors of Casein Kinase 2 alpha (CK2?) and are useful for the treatment and/or prevention of diseases and conditions in which CK2? activity is implicated, such as, for example, but not limited to, the treatment and/or prevention of proliferative disorders (e.g. cancer), viral infections, inflammation, diabetes, vascular and ischemic disorders, neurodegeneration and the regulation of circadian rhythm. The present invention also relates to pharmaceutical compositions comprising the compounds defined herein, to processes for synthesising these compounds and to their use for the treatment of diseases and/or conditions in which CK2? activity is implicated.

Abstract: The present disclosure relates generally to certain 6-azabenzimidazole compounds, pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions disclosed herein may be used for the treatment or prevention of diseases, disorders, or infections modifiable by hematopoietic progenitor kinase 1 (HPK1) inhibitors, such as HBV, HIV, cancer, and/or a hyper-proliferative disease.