Abstract: Arylsulfonamides of 4-heteroaryl-cyclohexyls, and their derivatives, are competitive and non-competitive inhibitors of the muscarinic acetylcholine receptor M5 (mAChR M5) and have utility in the treatment of psychiatric disorders such as substance-related misuse, substance-related disorder relapse, anxiety, depression, and psychosis.

Abstract: The present invention relates to a novel naphthyridinone derivative compound, a pharmaceutically acceptable salt thereof, a hydrate thereof, or a stereoisomer thereof, which are each relevant to a compound for inhibiting ENPP1, a composition for inhibiting ENPP1, and a method for inhibiting ENPP1.

Abstract: Compounds, compositions and their use in the treatment of a proliferative disease or condition such as a said proliferative disease or disorder is associated with a RAF gene mutation and/or a RAS gene mutation.

Abstract: Imidazo[4,5-c]quinoline compounds having a substituent that is attached at the N-1 position by a branched group, single enantiomers of the compounds, pharmaceutical compositions containing the compounds, and methods of making the compounds are disclosed. Methods of use of the compounds as immune response modifiers, for inducing cytokine biosynthesis in humans and animals, and in the treatment of diseases including infectious and neoplastic diseases are also disclosed.

Abstract: The invention relates to 4-((6-(2,2-Difluoroethyl)-8-(2-hydroxy-2-methylcyclopentyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl)amino)piperidine-1-sulfonamide or pharmaceutically acceptable salts thereof, to compositions containing them, to processes for their preparation, to intermediates used in such processes, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer. The disclosure also relates to its crystalline form 1, to pharmaceutical compositions comprising form 1, and to the use of form 1 for the treatment of cancers.

Abstract: The present invention is directed to inhibitors of Kirsten Rat sarcoma virus (KRAS), and more particularly to compounds of Formula I as well as compositions comprising Formula I and methods of using the compound of Formula I for the treatment or prevention of a disease, disorder, or medical condition mediated through KRAS, especially the KRAS mutant G12C.

Abstract: The present invention relates to: an anti-cancer pharmaceutical composition for targeting heat shock protein 70, containing an indoloquinazolidine alkaloid; and the like. The indoloquinazolidine alkaloid of the present invention inhibits the growth of tumors and inhibits the expression of HSP70 protein and the colony formation activity of cancer cells, and inhibits the growth of tumors in mouse models with xenografts of a cancer cell line and xenografts of patient-derived cancer, and inhibits the growth of cancer cells resistant to drugs such as pemetrexed, cisplatin, and paclitaxel, and thus is expected to be widely usable in the prevention and treatment of various types of cancer.

Abstract: The present application provides a nitrogen-containing polycyclic aromatic compound and its preparation method and application. The nitrogen-containing polycyclic aromatic compound has a structure of Formula I, has an excellent broad-spectrum anti-tumor activity, and shows an inhibitory activity comparable to cisplatin on cervical cancer cells, breast cancer cells, melanoma cells, lung cancer cells and myeloma cells. Compared with cisplatin, the compound also has lower toxicity, and may be used as a lead compound for the development of new anti-tumor drugs.

Abstract: A series of substituted imidazo[1,2-b]pyridazine derivatives as defined herein, being potent modulators of human IL-17 activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including inflammatory and autoimmune disorders.

Abstract: The present disclosure provides inhibitors of Janus Kinase 2 (JAK2) which may be used in the treatment of medical disorders such as cancer.

Abstract: Disclosed herein are heterocyclic compounds that inhibit the binding of menin and MLL or MLL fusion proteins. Also described are specific inhibitors of menin-MLL interaction. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the menin-MLL 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, leukemia and other diseases or conditions dependent on menin-MLL interaction.

Abstract: The disclosure relates to tricyclic heterocyclic derivatives as shown in Formula (I), to pharmaceutical compositions comprising them, to a process for their preparation, and their use as therapeutic agents.

Abstract: Novel PEG modified cyclic dipeptide compounds are disclosed. The modified cyclic dipeptide compounds contain a cyclic dipeptide and a biocompatible polymer attached to the cyclic dipeptide. The cyclic dipeptide may be proline-containing, hydroxyproline-, or histidine-containing cyclic dipeptide. In one embodiment, the cyclic dipeptide is a cyclo (-his-pro).

Abstract: A pharmaceutical intermediate including a first indole moiety which is associated with an optionally carboxylated hexahydroazepino moiety, an optionally carboxylated azonane moiety, or a second, optionally carboxylated indole moiety, having an alkyl, allyl, phenylallyl, cinnamyl, alkenyl, and/or alkyl-alkenyl substituent pendant from a nitrogen atom of the same.

Abstract: Provided herein are Bridged Compounds having the following structures: wherein R1a, R1b, R1c, R1d, R2a, R2b, R2c, R2d, R3a, R3b, R3c, R3d, R4, R5, R6, R7, R8, m1, m2, m3, n2, n3, n4, q, X1, X2, Y1, Y2, L1 and ring A are as defined herein, compositions comprising an effective amount of a Bridged Compound, and methods for treating or preventing various diseases, e.g., pancreatic cancer, or a condition treatable or preventable by inhibition of the function of KRAS protein. In another aspect, a Bridged Compound is useful for treating or preventing a condition treatable or preventable by inhibition of the function of KRAS protein with G12D mutation. In another aspect, a Bridged Compound is useful for treating or preventing a condition treatable or preventable by inhibition of a RAS/MAPK pathway.

Abstract: Provided herein are substituted fused quadracyclic compounds useful as inhibitors of MK2. The invention further provides pharmaceutical compositions of the compounds of the invention. The invention also provides medical uses of substituted fused quadracyclic compounds.

Abstract: Provided herein are compounds according to Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, and R7 are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) as well as the use of such compounds as M4 receptor agonists.

Abstract: The present disclosure relates to compositions and methods for treating cancers, immune disorders, and other preventive and therapeutic applications.

Abstract: Described is a compound having the structure (I), (II) or (V), Formulae(I), (II), (V), wherein R1 is —H, —CH2OH or —CH(OH)CH2OH; R2 is —H, —OH, or —CH2OH; R3 is —H, —OH, or —CH2OH; n is 0 or 1; p is 0 or 1; R10 is hydrogen or a hydrocarbon moiety with 1 to 20 carbon atoms, wherein each hydrogen atom of the hydrocarbon moiety may optionally be substituted with a C1-C4-alkyl group or a halogen atom; R is either —Z—F or Y and wherein Z is a hydrocarbon moiety with 0 to 10 carbon atoms, optionally substituted with 1 to 4 C1-C4-alkyl groups or 1 to 4 halogen atoms, and F is —COOH, —CH(COOH)2, —COOR4, —CHO, —CH(CHO)2, C2H3, —C2H, —N3, —NH2, —NHR7, —OH, —CH(CH2OH)2, wherein R4 is a C1-C4-alkyl group and R7 is a C1-C4-alkyl group and wherein Y is hydrogen or a linear, branched or cyclic organic residue having 1 to 20 carbon atoms with the proviso that if R is Y and n is 0 at least one of R1 or R2 is not hydrogen.

Abstract: Provided are a series of 5,6-dihydrothieno[3,4-h]quinazoline compounds as represented by formula (P) and pharmaceutically acceptable salts thereof, and the use of the compounds or pharmaceutically acceptable salts thereof in the preparation of solid tumor drugs, such as solid tumor drugs associated with selective PLK1 inhibitors.

Abstract: Provided are a fused tricyclic cyclin-dependent kinase inhibitor, and a preparation method therefor and a pharmaceutical use thereof. In particular, the structure of the fused tricyclic cyclin-dependent kinase inhibitor is shown in formula I, wherein substituents are defined in the description. The fused tricyclic cyclin-dependent kinase inhibitor is used for preventing and/or treating cyclin-dependent kinase related diseases, in particular cancers.

Abstract: The present invention relates to certain diaryl macrocyclic compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating cancer, pain, neurological diseases, autoimmune diseases, and inflammation.

Abstract: The invention relates to compounds of formula (I) wherein the variables are as defined in the specification. It also relates to the use of compounds of formula (I) (I); and to agrochemical or veterinary compositions comprising compounds of formula (I).

Abstract: Disclosed herein are crystalline and amorphous forms of (1S,3?R,6?R,7?S,8?E,11?S,12?R)-6-chloro-7?-methoxy-11?,12?-dimethyl-3,4-dihydro-2H, 15?H-spiro[naphthalene-1,22?-[20]oxa[13]thia[1,14]diazatetracyclo[14.7.2.03,6,019,24]pentacosa[8,16,18,24]tetraen]-15?-one 13?,13?-dioxide (AMG 176): and salts and hydrates thereof. Also disclosed are methods of making the crystalline and amorphous forms, and methods of treating diseases and disorders with the crystalline and amorphous forms.

Abstract: The present invention provides processes for preparing 7H-pyrrolo[2,3-d]pyrimidine derivatives, which are useful as a Janus kinase (JAK) inhibitor, intermediates thereof, and processes for preparing the intermediates. The present invention provides processes for preparing 3-[(3S,4R)-3-methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1,6-diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile using salts of (3S,4R)-1-benzyl-3-methyl-1,6-diazaspiro[3.4]octane with organic acids.

Abstract: An organic compound, a light-emitting component, and a display panel are disclosed. The organic compound has a structure shown as general formula (1): This organic compound can enhance conjugated effect and resonance effect of materials applied into the light-emitting component by having a heterocyclic group and an amino group at a same time. Therefore, material performances can be improved, a luminous efficiency of the light-emitting component can be improved, and a light-emitting service life of the light-emitting component can be extended.

Abstract: Anthraquinone-based covalent organic frameworks; methods for preparing anthraquinone-based covalent organic frameworks; solid electrolyte interphases including the anthraquinone-based covalent organic frameworks; and electrochemical devices including the solid electrolyte interphases. The solid electrolyte interphases can exhibit enhanced transport of Li+. Battery cells including the solid electrolyte interphase exhibit improved reversible capacities.

Abstract: Described is a deuterated compound, and preparation method and use thereof The deuterated compound I has a structure as shown in Formula (I), wherein A is H or D, and at least one of eight As is D; M is H or an alkali metal, an alkaline earth metal, or an ammonium radical. The present invention provides use of the deuterated compound I as an internal standard for measuring the content of a metabolite II in a biological sample, wherein the metabolite II has a structure as shown in a Formula (II); wherein A is H; M is H or an alkali metal, an alkaline earth metal, or an ammonium radical. The present invention uses the deuterated compound I as an internal standard to quantitatively analysis the content of metabolite II at lower content in biological samples, which can not only meet the requirements for the lower limit of quantitation, but also meet the requirements for DMPK studies in clinical trials.

Abstract: PSMA binding scaffolds with radioiodinated, radiobrominated and radioastatinated labeled prosthetic groups are disclosed. Pharmaceutical compositions and methods of treating PSMA expressing cells or tumors also are disclosed.

Abstract: An organometallic compound represented by Formula 1: M1(L1)n1(L2)n2??Formula 1 wherein, M1 is a transition metal, L1 is a ligand represented by Formula 1A, L2 is a ligand represented by Formula 1B, and n1 and n2 are each independently 1 or 2, wherein X1 is C or N; and X2 is C or N; Y1 is O, S, or Se; ring CY1 is a C5-C30 carbocyclic group or a C1-C30 heterocyclic group; * and *? each indicate a binding site to M1; and the remaining substituent groups are as defined herein.

Abstract: A compound comprising a ligand of LA of Formula I, is provided with variables as defined herein. Formulations, OLEDs, and consumer products including the compound are also disclosed.

Abstract: The present disclosure concerns cucurbit[n]uril (CB) complexes of cucurbit[8]uril (CB[8]) and/or cucurbit[7]uril (CB[7]) that secure or host platinum conjugated terpyridines. The platinum center can further secure a protein through the thiol of a cysteine or an imidazole of a histidine therein. Additional CBs can secure the peptide through phenyl side chains. CB[8] will secure a dimer of platinum-terpyridines in a head-to-head alignment or a peptide dimer through a head-to-tail alignment. The application of multiple CBs allows for varying CB complex geometries. Also contemplated are methods of using the platinum-terpyridines to selectively bind cysteine rich proteins, such as cysteine proteases.

Abstract: The present invention relates to an antiviral application of nucleoside analogs. Specifically, the present invention relates to uses of nucleoside analogs and a pharmaceutical composition thereof as: (a) inhibitors for inhibiting the replication of coronaviruses, influenza viruses, respiratory syncytial viruses, flaviviridae viruses, filoviridae viruses and/or porcine epidemic diarrhea virus (PEDV); and/or (b) medicines for treating and/or preventing and mitigating diseases caused by coronavirus, influenza virus, respiratory syncytial virus, flaviviridae virus, filoviridae virus and/or porcine epidemic diarrhea virus (PEDV) infections. The nucleoside analogs according to the invention may treat and/or prevent and mitigate respiratory infection, pneumonia (COVID-19) and other related diseases caused by 2019 novel coronavirus infection.

Abstract: A process is provided for the synthesis of an intermediate which is useful in the synthesis of E-selectin inhibitors. Also provided are useful intermediates obtained from the process.

Abstract: The present application is directed to, in part, nucleotide analogs with a novel design of a 3?-OH reversible terminator that comprises an enzyme-cleavable linkage.

Abstract: Methods and compositions are provided for oligonucleotides that bind targets of interest. The targets include cells and microvesicles, such as those derived from various diseases. The oligonucleotides can be used for diagnostic and therapeutic purposes. The target of the oligonucleotides can be a target such as PARP1, HIST1H1B, HIST1H1D, NCL, FBL, SFPQ, RPL12, ACTB, HIST1H4A, SSBP1, NONO, H2AFJ, and DDX21, or a complex, subunit or fragment thereof.

Abstract: Provided are compounds and methods which may be useful as inhibitors of CD73 for the treatment or prevention of cancer.

Abstract: Provided are compounds which may be useful as inhibitors of CD73 for the treatment or prevention of cancer.

Abstract: The present disclosure, in some aspects, is directed to nucleic acid purification methods using a water-immiscible solvent wash. In other aspects, the present disclosure is directed to kits, components, and compositions (such as consumables) useful for the nucleic acid purification methods described herein.

Abstract: Provided herein are methods and compositions for synthesizing 5?Capped RNAs wherein the initiating capped oligonucleotide primers have the general form m7Gppp[N2?Ome]n[N]m wherein m7G is N7-methylated guanosine or any guanosine analog, N is any natural, modified or unnatural nucleoside, “n” can be any integer from 0 to 4 and “m” can be an integer from 1 to 9.

Abstract: The invention relates to single stranded DNA inhibitors of APOBEC3 enzymes and uses thereof. The compounds of the invention comprise ?-D-5-O-phosphato-2-deoxyribofuranosyl analogues of nucleoside-like inhibitors of cytidine deaminase, flanked by oligonucleotide sequences which may be cross-linked. The compounds of the invention may have therapeutic application against diseases and conditions in which inhibition of a human cytidine deaminase of the APOBEC3 family would be beneficial.

Abstract: The present invention provides compounds of Formula I, pharmaceutical compositions comprising these compounds and methods of using these compounds to prevent or treat FXR-mediated or TGR5-mediated diseases or conditions.

Abstract: The invention relates to salts of Compound 1, crystalline forms thereof, methods of their preparation, pharmaceutical compositions thereof and methods of their use

Abstract: Disclosed herein are compounds of Formula (I-A), wherein the vari-ables are defined herein. Also provided are pharmaceutical compositions thereof. In some aspects, the compounds and compositions provided herein may be used as antioxidant inflammation modulators. In some aspects, the present disclosure provides methods wherein the compounds and composition described herein are used for the treatment of diseases and disorders associated with inflammation and cancer.

Abstract: Single cell protein (SCP) is produced by applying a voltage to a microbial electrolysis cell (MEC) under anaerobic conditions for a period of time, whereby SCP is produced. The MEC includes a cathode comprising a hydrogen evolution reaction material, an anode comprising a biofilm on a carbon support, an electrolyte comprising carbon, nitrogen, and phosphorus, and a Methanococcus or Acetobacterium species in the electrolyte.

Abstract: A method of isolating an antibody is disclosed. The method comprises contacting a hydrophobic chelator, a non-ionic detergent and metal ions so as to generate an aggregate comprising the hydrophobic chelator, the detergent and the metal ions; and contacting the aggregate with a medium comprising the antibody under conditions that allow partitioning of the antibody into the aggregate. Kits for isolating the antibody are also disclosed.

Abstract: A method and system for integrated and continuous viral filtration and biological product concentration, including an initial purification system coupled to a final purification system. The initial purification system includes a viral reduction filtration (VRF) skid, while the final purification system includes a single-pass tangential filtration-diafiltration (SPTFF-DF) skid.

Abstract: Disclosed are various crystalline salt forms of Boc-D-Arg-DMT-Lys(Boc)-Phe-NH2.

Abstract: A compound of formula (I) or formula (II) including tautomeric or stereochemically isomeric forms thereof, wherein: R1 represents C1-20 alkyl, C2-20 alkenyl, C6-20 aryl, or C4-20 heterocyclyl, each optionally substituted with one or more Y groups, R2a to R2l each independently represents H, C1-10 alkyl, C2-10 alkenyl, C6-12 aryl, or C4-12 heterocyclyl, each optionally substituted with one or more Y groups, R3 represents H, C1-10 alkyl, C2-10 alkenyl, C6-12 aryl, or C4-12 heterocyclyl, each optionally substituted with one or more Y groups, X represents NH, S or O, each Y independently represents cyano, halogen, N3, —C(O)RZ, —C(0)0Rz, —0C(0)Rz, —C(0)NHZ, —NHC(O)Rz, —NHC(0)NHRZ, —NHC(NH)NHRZ, —NCH(0)0Rz, -0C(0)NHRz, -0S(0)2RZ, —S(0)2NHRZ, —NHS(0)2RZ, —SRZ, —NRZZ or —ORz and each Rz independently represents H, C1-10 alkyl, C2-10 alkenyl, C6-10 aryl, or C4-10 heterocyclyl; or an N-oxide thereof or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof; and wherein formula (I) e

Abstract: The present disclosure provides compounds of Formula (I): or a pharmaceutically acceptable salt, solvate, or tautomer thereof, and uses of the same in treating a disease or disorder (e.g., cancer or fibrosis).