Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.

Abstract: The present invention relates to a biaryl derivative compound, which exhibits the activity of a diacylglycerol acyltransferase 2 (DGAT2) inhibitor and is represented by chemical formula (1), a pharmaceutical composition comprising same as an active ingredient, and a use thereof.

Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses a molecule having the following formula.

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: Described herein, inter alia, are compounds for treating cancer and methods of use. This disclosure features chemical entities (e.g., small hairpin RNAs (shRNAs), micro RNA (miRNAs), small interfering RNA (siRNAs), small molecule inhibitors, antisense nucleic acids, peptides, viruses, CRISPR-sgRNAs, or combinations thereof) that inhibit one or more of m6A writers (e.g., methyltransferase like 3 (Mettl3 or MT-A70) or methyltransferase like-14 (Mettl14)), m6Am writers (e.g., phosphorylated CTD interacting factor I (PCIF 1), or Mettl3/14), m6A erasers (e.g., fat-mass and obesity-associated protein (FTO) or ALKB homolog 5 (ALKBH5)), m6Am erasers (e.g., FTO), m6A readers (e.g., YTH domain-containing family proteins (YTHs)), YTF domain family member 1 (YTHDF 1), YTF domain family member 2 (YTHDF 2), YTF domain family member 3 (YTHDF 3), or tyrosine-protein phosphatase non-receptor type 2 (PTPN2).

Abstract: Provided are a crystal form of a free base or a pharmaceutically acceptable salt of (R)-N-(4-(chlorodifluoromethoxy)phenyl)-6-(3-fluoropyrrolidin-1-yl)-5-(pyrazin-2-yl)nicotinamide (compound A), a preparation method therefor, and use of the compound in preparation of drugs for treating diseases mediated by Bcr-Abl kinase and mutants thereof, such as chronic granulocytic leukemia. Also provided are a method for preparing compound A, and a preparation containing compound A.

Abstract: The present invention relates to compounds of general formula (I), tautomers, stereoisomers, N-oxides, pharmaceutically acceptable salts and pro-drug thereof, to processes for their preparation, to pharmaceutical compositions containing such compounds and to their use in therapy: wherein: a dashed line indicates an optional bond; X represents: a 5- or 6-membered, unsaturated heterocyclic group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g. C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), C1-6 alkoxy (e.g. C1-3 alkoxy), —CN, —NO2, —N(R)2, and —SO2R (where each R is independently H or C1-6 alkyl, e.g. H or C1-3 alkyl); a C3-5 cycloalkyl group optionally substituted by one or more (e.g. 1 or 2) substituents independently selected from C1-6 alkyl (preferably C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); or an aryl group optionally substituted by one or more (e.g.

Abstract: Disclosed herein are compounds and compositions having potency in the modulation of Myc family proteins. Such compounds and compositions can be used in the treatment of proliferative diseases, such as cancer, or in the treatment of disease where modulation of Myc family proteins is desired. Also disclosed herein are methods of using said compounds and compositions.

Abstract: The present disclosure provides a compound of a specific chemical structure or a pharmaceutically acceptable salt thereof, which has the activity of inhibiting and/or degrading mutant EGFR protein. The present disclosure also provides a composition comprising such a compound or a pharmaceutically acceptable salt thereof. The present disclosure provides a pharmaceutical use of a compound according to the present disclosure, a salt thereof, and a composition comprising same for the treatment or prevention of cancer with EGFR mutation, especially lung cancer. The present disclosure also provides a method for treatment or prevention of EGFR mutation cancer, especially lung cancer, the method comprising administering an effective amount of the compound according to the present invention, a salt thereof, or a composition containing same to a subject in need of treatment.

Abstract: The present invention provides heterocyclic compounds of formula (I), which are therapeutically useful as CBP/EP300 inhibitors. These compounds are useful in the treatment and/or prevention of diseases or disorders mediated by CBP and/or EP300 in an individual. The present invention also provides preparation of the compounds and pharmaceutical compositions comprising at least one of the compounds of formula (I) or a pharmaceutically acceptable salt, or a stereoisomer or a tautomer, an N-oxide or an ester thereof.

Abstract: Disclosed are inhibitors for the ?-catenin/BCL9 interaction. The inhibitors are selective for ?-catenin/BCL9 over ?-catenin/cadherin in-teractions. Methods of using the disclosed compounds to treat cancer are also disclosed.

Abstract: A compound of formula I wherein A, X, Y, Z, R1 and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.

Abstract: Disclosed are solid forms of a Cot (cancer Osaka thyroid) inhibitor and corresponding methods of preparation thereof, wherein the Cot inhibitor has the following formula:

Abstract: Compounds are provided that are useful as immunomodulators. The compounds have the Formula (I) including stereoisomers and pharmaceutically acceptable salts thereof, wherein R2a, R2b, R3, R3a, R4, R6, R7, R8, A, Z, X1 and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

Abstract: The present disclosure includes azetidinyl tryptamines and methods of treating psychiatric disorders with such compounds. Also provided are pharmaceutical compositions that include azetidinyl tryptamines.

Abstract: This invention relates to novel salts and crystal forms of 2-[3-({1-[2-(dimethylamino)ethyl]-2-(2,2-dimethylpropyl)-1H-1,3-benzodiazol-5-yl}sulfonyl)azetidin-1-yl]ethan-1-ol, simply abbreviated as Compound A, which is a selective CB2 receptor agonist. The present invention provides a salt of Compound A, a crystal form thereof, a method for preparing the said salt and a pharmaceutical composition thereof and its use. The salts of Compound A of the present invention show good pharmaceutical formulation properties such as high aqueous solubility, good crystallinity, high melting point, good chemical and physical stability, or non-deliquescent.

Abstract: The present disclosure provides a compound of formula (I), or an isotopically labeled product, an enantiomer, a diastereomer or a pharmaceutically acceptable salt thereof; a pharmaceutical composition comprising a compound of formula (I); and use of a compound of formula (I) or a pharmaceutical composition thereof in the treatment of diabetes mellitus and related symptoms.

Abstract: Disclosed herein, inter alia, are compounds and methods of use thereof for the modulation of certain chemokine receptor activity.

Abstract: Compounds and methods for purifying oligonucleotides such as RNA and DNA. A target oligonucleotide is reacted with an orthoester linker comprising an affinity tag to form an orthoester oligonucleotide-orthoester linker conjugate which is subjected to a purification technique to separate the target oligonucleotide from impurities such as truncated oligonucleotides. The orthoester linker can be then removed under mild conditions to generate the target oligonucleotide in high purity.

Abstract: The present invention provides a novel group of active peptide compounds based on the psychoactive safrylamine compounds MDMA, MDA, MMDA-2, and MDAI. Thereby, the invention provides for improved pharmacokinetic properties during uptake of the safrylamines, as well as reduced side effects resulting from the metabolites thus formed. Due to the affinity of the novel safrylamine derivatives for the 5-HT2a-receptor, the invention can find use in numerous forms of therapy, such as against depression or posttraumatic stress disorder (PTSD).

Abstract: The present application provides compounds that may be used as a glucagon-like peptide-1 receptors (GLP-1R) agonist, or stereoisomers, tautomers, or pharmaceutically acceptable salts of any of the foregoing. Also provided are pharmaceutical compositions containing such compounds, or stereoisomers, tautomers, or pharmaceutically acceptable salts of any of the foregoing. Methods of prepare these compounds and compositions and method of using them to treat or present a disease or a condition mediated by GLP-1R.

Abstract: Disclosed are a fused tricyclic derivative and a pharmaceutical application thereof. Specifically disclosed are a compound represented by formula (III) and a pharmaceutically acceptable salt thereof.

Abstract: Provided herein are compounds that selectively inhibit HDAC6, a protein whose activity is associated with a variety of diseases (e.g., cancer, neurological disorders). Also provided are pharmaceutical compositions and kits comprising the compounds, and methods of treating HDAC6-related diseases and disorders (e.g., Alzheimer's disease, cancer) with the compounds in a subject, by administering the compounds and/or compositions described herein.

Abstract: A method of treating and/or preventing disease involving retinal pigment epithelium, including administering compound of formula (I) or a pharmaceutically acceptable salt, a racemic mixture, a corresponding enantiomer or a corresponding diastereomer thereof, wherein: R1, R11 and R12 are independently selected from the group consisting of hydrogen, fluoro, chloro, methoxy, trifluoromethyl, methyl and difluoromethoxy, whereby at least one of R1, R11 and R12 is not hydrogen, B is selected from the group consisting of a residue of formula (II), (III), (IV), (V), (VI) and (VII) wherein,“*” denotes point of attachment to remainder of the molecule, and R2, R3, R4, R5, R2I, R3I, R4I, R5I, R2II, R3II, R4II, R5II, R2III, R3III, R4III, R5III, R2IV, R3IV, R4IV, R5IV, R2V, R3V,R4V, R5V are independently selected from the group consisting of hydrogen, a linear or branched alkyl having 1 to 3 carbon atoms, fluoro, chloro, bromo, methoxy, ethoxy, propoxy, trifluoromethyl and difluoromethoxy

Abstract: The present invention relates to a pharmaceutical composition comprising a compound of the present invention, an isomer thereof, a hydrate thereof, a solvate thereof, or a pharmaceutically acceptable salt thereof as an active ingredient for prevention or treatment of cancer. The compound exhibits high inhibitory activity against epidermal growth factor receptor (EGFR) mutants or at least one of the wild-type or mutant ErbB2 and ErbB4 and as such, can be advantageously used for treatment of the cancer expressing same.

Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.

Abstract: 1. The present invention relates to the crystal of compound X7 hydrochloride and its preparation method and application. The 2? diffraction angle of the X-ray powder diffraction diagram of the crystal of compound X7 hydrochloride exhibits characteristic diffraction peaks in the range of 5°˜35°. The crystal of the compound X7 hydrochloride has better physical and chemical properties.

Abstract: Disclosed are fused imidazole derivatives, preparation methods therefor and medical uses thereof. Specifically, the present disclosure relates to a fused imidazole derivative as shown in general formula (IM), a preparation method therefor, a pharmaceutical composition containing the derivative, and the use of same as a therapeutic agent, in particular the use thereof as a GLP-1 receptor agonist, and the use thereof in the preparation of drugs for the treatment and/or prevention of diabetes.

Abstract: The present application provides compounds that may be used as a glucagon-like peptide-1 receptors (GLP-1R) agonist, or pharmaceutically acceptable salts thereof. Also provided are pharmaceutical compositions containing such compounds, or pharmaceutically acceptable salts thereof. Methods of preparing these compounds and compositions, and methods of using these compounds and compositions to treat or prevent a disease or a condition mediated by GLP-1R, are also provided.

Abstract: A crystal form of an azaindole derivative and a preparation method thereof are disclosed.

Abstract: Disclosed herein are novel bifunctional compounds formed by conjugating BTK inhibitor moieties with E3 ligase Ligand moieties, which function to recruit targeted proteins to E3 ubiquitin ligase for degradation, and methods of preparation and uses thereof.

Abstract: The present disclosure relates to novel compounds that are capable of inhibiting the mitochondrial pyruvate carrier and promoting hair growth. The disclosure further relates to methods of promoting hair growth or treating conditions or disorders affecting hair growth, such as baldness or alopecia.

Abstract: Compounds of formula (I), process for their production and their use as pharmaceuticals.

Abstract: A heteroaromatic ring compound as a RET kinase inhibitor, and the preparation and the use thereof, wherein the compound is a compound having the structure of formula (I) or a pharmaceutically acceptable salt thereof. The compound or a salt thereof can be used for treating or preventing diseases or conditions by targeting receptors of fused and mutated forms of the RET gene, can effectively inhibit the growth of multiple tumor cells, produces an inhibitory effect on a RET gene fusion mutation and other proteases, and can be used for preparing an anti-tumor drug.

Abstract: Disclosed are compounds of Formulas (I) and (II): or a salt thereof, wherein X, Y, Q1, Q2, G, R1, and R3 are defined N herein. Also disclosed are methods of using such compounds as inhibitors of TLR9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing fibrotic diseases.

Abstract: This disclosure relates to GLP-1 agonists of Formula (I), including pharmaceutically acceptable salts and solvates thereof, and pharmaceutical compositions including the same.

Abstract: The invention provides novel azaindolylpyridone and diazaindolylpyridone compounds of formula (I), pharmaceutical compositions containing such compounds, and methods for using such compounds in treatment of diseases including cancer, type II diabetes, inflammatory diseases, autoimmune diseases, neurodegenerative disorders, cardiovascular disorders and viral infections; wherein R2, R3 and X are as defined in the specification.

Abstract: The invention provides compounds of formula (I): where the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions comprising such compounds and methods of using such compounds to treat respiratory diseases.

Abstract: Polycystic ovary syndrome (PCOS) is characterized by elevated levels of androgens, cysts in the ovaries, and irregular periods. Women with PCOS present with additional symptoms, including hirsutism, alopecia, acne, infertility, weight gain, fatigue, depression and mood changes. The present disclosure provides new compounds, salts, compositions and uses thereof in the treatment of PCOS due to elevated adrenal androgens. Further, the present disclosure provides methods for treating PCOS due to elevated adrenal androgens.

Abstract: The invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein n, R1, R2, R3, R4 and R5 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.

Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3, Z, A1, L and A2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.

Abstract: The present disclosure relates to agonists of interferon alpha and beta receptor subunit 2 (IFNAR2) for use in the treatment or prevention of viral disease, particularly COVID-19. In particular embodiments, COVID-19 is associated with pneumonia or acute respiratory distress syndrome (ARDS). In other aspects, the subject being treated is undergoing extra-corporeal membrane oxygenation, mechanical ventilation, non-invasive ventilation, receiving oxygen therapy or receiving antiviral or steroid treatment.

Abstract: Disclosed herein are ring-in-ring photoluminescent complexes comprising a host cyclophane and a guest cyclophane threaded through the host cyclophane and methods of using and making the same. Further disclosed herein a method for tuning photo-luminescence, the method comprising providing a host cyclophane and a guest cyclophane, contacting the guest cyclophane with the host cyclophane thereby forming the ring-in-ring photoluminescent complex.

Abstract: Certain embodiments are directed to the use of chemical compounds that inhibit migration and growth of cancer cells.

Abstract: The present invention relates to a process for the preparation of ticagrelor, which provides a product of high purity, in particular, with no detectable levels of Nnitrosmine impurities. The process comprises a first step of treating 2- [[(3aR,4S,6R,6aS)-6-[[5-amino-6-chloro-2-(propylthio)-4-pyrimidinyl]amino]tetrahydro-2,2-dimethyl-4H-cyclopenta-1,3-dioxol-4-yl]oxy]ethanol starting material with sodium nitrite, followed by acidic washing; in a second step, the 2-[[(3aR,4S,6R,6aS)-6-[7-chloro-5-(propylthio)-3H-1,2, 3-triazolo[4,5-d]pyrimidin-3-yl]tetrahydro-2,2-dimethyl-4H- cyclopenta-1,3-dioxol-4-yl]oxy]ethanol obtained in the previous step is coupled with trans-(1 fl,2S)-2-(3,4-difluorophenyl)cyclopropylamine, and the reaction is followed by a first washing at basic pH a second washing at acidic pH; and in an third step, the compound obtained in the previous step is deprotected by treatment with mineral acid, followed by acidic washing.

Abstract: The present invention provides compounds of the structural Formula (I) and pharmaceutically acceptable salts thereof, wherein, are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.

Abstract: The present disclosure encompasses solid state forms of AT-001, in embodiments crystalline polymorphs of AT-001 or salts or co-crystals of AT-001, processes for preparation thereof, and pharmaceutical compositions thereof.

Abstract: Certain aspects of the present invention are directed to improved processes for preparing enantiomerically enriched intermediates for the synthesis of ruxolitinib and deuterated forms of ruxolitinib. Certain aspects are also directed to deuterated intermediates useful in the synthesis of deuterated forms of ruxolitinib. Certain aspects are also directed to reaction mixtures for preparing enantiomerically enriched intermediates useful in the synthesis of ruxolitinib and deuterated forms of ruxolitinib.

Abstract: Disclosed herein are imidazotriazine and pyrrolopyrimidine derivatives or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof useful as a G12C inhibitors, and a pharmaceutical composition comprising the same. Also disclosed herein is a method of treating cancer using the imidazotriazine and pyrrolopyrimidine derivatives or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof as G12C inhibitors.