Abstract: Disclosed herein are novel cycloalka[b]heteroaryl compounds having CX3CR1/fractalkine receptor (CX3CR1) agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment or prophylaxis of diseases associated with CX3CR1 receptor activity in animals, in particular humans.

Abstract: Disclosed are inhibitors for TAF1. The TAF1 inhibitors are compounds having a structure according to one of the Formula described herein. Methods of using the disclosed compounds to treat proliferative disorders are also disclosed.

Abstract: Described herein are compounds of Formula I, wherein the variables are defined herein, their use as HSD17B13 inhibitors and/or degraders, pharmaceutical compositions containing such compounds and their use to treat, for example, NAFLD and NASH.

Abstract: The present invention relates to a series of fused ring derivatives containing 1,4-oxazepane and a preparation method therefor, and in particular relates to a compound as shown in formula (II) and a pharmaceutically acceptable salt thereof.

Abstract: Provided herein is a process for the preparation of (R)-N-(5-(5-ethyl-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-yl)-1-methyl-1H-pyrazole-4-carboxamide, intermediates thereof, and salts of the foregoing.

Abstract: The present invention relates to a 6-(isooxazolidin-2-yl)-N-phenylpyrimidin-4-amine derivative, and a pharmaceutical composition for preventing or treating cancer comprising the compound as an effective component. The compound exhibits high inhibitory activity against an epidermal growth factor receptor (EGFR) variant, or wild-type or variants of one or more of ERBB2 and ERBB4, and thus may be usefully used in the treatment of cancers in which same are expressed. In particular, the compound exhibits excellent inhibitory activity on proliferation of lung cancer cell lines, and thus can be usefully used in the treatment of lung cancer.

Abstract: Provided are, inter alia, compounds having a structure of Formulae (X) to (XVII), or a subordinate structure thereof, composition including the same and methods of use.

Abstract: The present invention relates to compounds of Formulas A-D, I-IV and Z, their use as activators of long form cyclic nucleotide phosphodiesterase-4 (PDE4) enzymes (isoforms) and to these compounds for use in a method for the treatment or prevention of disorders requiring a reduction of second messenger responses mediated by cyclic 3?,5?-adenosine monophosphate (cAMP).

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: The present invention relates to a composition for preventing or treating diseases caused by mitochondrial dysfunction, containing, as an active ingredient, an isoquinoline derivative compound represented by chemical formula 1, or a pharmaceutically acceptable salt thereof, and does not induce mitochondrial damage, unlike conventional mitochondrial toxins such as CCCP, and specifically and excellently promotes the activity of mitophagy to alleviate mitochondrial disfunction, and thus can be effectively used in the treatment of diseases caused by mitochondrial dysfunction.

Abstract: The present invention is directed to compounds according to Formula I and the pharmaceutically acceptable salts thereof. The compounds can be used as modulators of Estrogen-related Receptor alpha (ERR?) and have utility in the treatment of ERR?-mediated diseases or conditions.

Abstract: Disclosed in the present invention are a compound having a BRD4 inhibitory activity, a preparation method therefor and the use thereof. The structure of the compound having the BRD4 inhibitory activity of the present invention is as shown in formula I, and the definition of each substituent is as described in the description and claims. The compound of the present invention has a high bromodomain protein inhibitory activity, in particular a BRD4-targeting inhibitory activity, and can be used for the treatment and/or prevention of related diseases mediated by bromodomain proteins.

Abstract: The present invention relates to a process for preparing acyloxymethyl esters of (4S)-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxylic acid of the formula (IIa) by optical resolution of the compound of the formula (II) using a hydrolase. The invention also relates to a process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (Ia), wherein the process comprises the optical resolution of the compound of the formula (II) using a hydrolase. The invention additionally also relates to the use of a hydrolase in a process for preparing a compound of formula (IIa). The invention further relates to the use of a hydrolase in a process for preparing a compound of formula (Ia).

Abstract: Provided herein are compounds, compositions, and methods useful for modulating the activity of GCN2 and for treating related conditions, diseases, and disorders (e.g., cancer and neurodegenerative diseases).

Abstract: A compound, as represented by formula I, as a TLR7 agonist, a method for preparing the compound, and the use of the compound in treating diseases mediated by the TLR7 agonist are provided. Studies on the activity of a human-derived receptor, a TLR7 agonist, show that compounds have a strong agonistic effect on the human-derived receptor, TLR7, and can be used as a foreground compound for treating diseases mediated by the TLR7 agonist.

Abstract: The present disclosure is directed to solid and salt forms of inhibitors of the CBP/p300 family of bromodomains made up of salts and crystalline forms of Formula (I). The compounds can be useful in the treatment of disease or disorders associated with the inhibition of the CBP/p300 family of bromodomains. For instance, the disclosure is concerned with compounds and compositions for inhibition of the CBP/p300 family of bromodomains, methods of treating diseases or disorders associated with the inhibition of CBP/p300 family of bromodomains (e.g., certain forms of cancer), and methods of synthesis of these compounds.

Abstract: The present invention relates to methods and compositions for the treatment of BAF-related disorders such as cancers and viral infections.

Abstract: The present disclosure is directed to inhibitors of the CBP/p300 family of bromodomains. The compounds can be useful in the treatment of disease or disorders associated with the inhibition of the CBP/p300 family of bromodomains. For instance, the disclosure is concerned with compounds and compositions for inhibition of the CBP/p300 family of bromodomains, methods of treating, preventing, or ameliorating diseases or disorders associated with the inhibition of CBP/p300 family of bromodomains, and methods of synthesis of these compounds.

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

Abstract: Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), or a pharmaceutically acceptable salt thereof.

Abstract: The invention provides a crystalline imidazo[4,5-b]pyridine compound, pharmaceutical compositions, methods of inhibiting tropomyosin-related kinase and/or c-FMS, and methods of treating medical diseases and conditions, such as pain.

Abstract: Provided herein are 2-substituted bicyclo[1.1.1]pentane (BCP) compounds, as well as methods of making the 2-substituted BCP compounds and methods of derivatizing the 2-substituted BCP compounds, particularly at the 2-position. The 2-substituted BCP compounds described herein are useful building blocks in the synthesis of a variety of products, including pharmaceuticals, polymers, liquid crystals, monolayers and supramolecular structures.

Abstract: The present application provides tricyclic urea compounds that modulate the activity of the V617F variant of JAK2, which are useful in the treatment of various diseases, including cancer.

Abstract: The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where R1, A1, A2 and A3 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent DNA-PK mediated disease, including cancer. The specification further relates to pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating DNA-PK mediated disease, including cancer, using such compounds and salts.

Abstract: Disclosed are compounds of formula (I) below or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof: in which each of variables each of variables R, R1, R2, X1, X2, X3 and n is defined herein. Also disclosed is a method for treating a cancer with a compound of formula (I) or a salt thereof and a pharmaceutical composition containing same.

Abstract: The invention relates to a method for preparing racemic (4R,4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I) from the enantiomers (Ia) or (Ib); a method for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (Ia); a method for preparing racemic (4R,4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I) from the pyridine of the formula (II). The objects of the invention have in common the irradiation of the compound of the formulae (Ia), (Ib) and/or (II) with light in a suitable solvent, or solvent mixture, in the presence of a base. The compounds of the formulae (Ia), (Ib) and/or (II) are intermediates, by-products or target compounds in the synthesis of finerenone (compound according to formula (Ia)).

Abstract: Disclosed are compounds useful in the treatment of neurological disorders. The compounds described herein, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological diseases.

Abstract: Compounds and methods of using said compounds, singly or in combination with additional agents, and salts or pharmaceutical compositions of said compounds for the treatment of viral infections are disclosed.

Abstract: The present disclosure relates to compounds of Formula (I), and the pharmaceutically A—(CH2)m—X—Y—Z—B1??I, acceptable salts and solvates thereof, wherein A, m, X, Y, Z, and B1 are as defined as set forth in the specification. The present disclosure also relates to uses of the compounds, e.g., in treating or preventing a condition or disorder responsive to the degradation of CBP/P300 proteins (e.g., cancer).

Abstract: Disclosed is a compound of Formula (I), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions comprising thereof. Also disclosed is a method of treating PI3K? related disorders or diseases by using the compound disclosed herein.

Abstract: The inventive compounds are small molecule therapeutics that are potent inhibitors of USP7 activity. The invention also provides pharmaceutical compositions comprising the compounds, and methods for using the compounds for treating or preventing a disease, disorder, or condition associated with USP7 activity.

Abstract: Described are coelenterazine analogues, methods for making the analogues, kits comprising the analogues, and methods of using the compounds for the detection of luminescence in luciferase-based assays. For example, the compounds may be used for in vivo imaging.

Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient are disclosed.

Abstract: The invention provides pyridinylsulfonamide compounds, pharmaceutical compositions, their use for inhibiting mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1), and their use in the treatment of a disease or condition, such as a proliferative disorder, inflammatory disorder, or autoimmune disorder.

Abstract: [Problem] A compound useful as an active ingredient of a pharmaceutical composition for treating pancreatic cancer is provided. [Solution] The present inventors have studied about a compound that is useful as an active ingredient of a pharmaceutical composition for treating pancreatic cancer and have found that a 4-aminoquinazoline compound has an excellent G12D mutant KRAS inhibition activity and can be used as a therapeutic agent for pancreatic cancer, thus completing the present invention. The 4-aminoquinazoline compound of the present invention or a salt thereof can be used as a therapeutic agent for pancreatic cancer.

Abstract: A compound of the following general formula [I]: wherein each symbol has the same meaning as defined herein, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutical use of the same in treating organ transplant rejection, graft versus host reaction after transplantation, autoimmune disease, allergic disease and chronic myeloproliferative disease.

Abstract: Described herein are compounds that are inhibitors of autophagy and their use in the treatment of disorders such as cancers.

Abstract: This invention is in the area of cell cycle inhibiting compounds for the treatment of disorders involving abnormal cellular proliferation, and include selective CDK2 inhibitors for medical therapy and their pharmaceutically acceptable salts and compositions.

Abstract: The present disclosure provides bicyclic pyridine derivatives. A compound represented by formula I: or a pharmaceutically acceptable salt thereof, wherein X is a oxygen atom, sulfur atom, NR, or CR?R?, n is 0 or 1, R1, R2a, R2b, R2c, R2d, R, R? and R? are each independently a hydrogen atom, a halogen atom, optionally substituted C1-6 alkyl, or an optionally substituted C6-10 aryl, or two of R2a, R2b, R2c, R2d, R, R?, and R?, together with a carbon atom or a nitrogen atom to which they are attached, form a 3- to 6-membered saturated carbocyclic ring or saturated heterocyclic ring, and R3a, R3b, R3c and R5a and R5b, are as defined in the description.

Abstract: Disclosed herein are compounds of Formula I?. Compounds of Formula I? inhibit, regulate and/or modulate kinase receptor, particularly Axl and Mer signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.

Abstract: The present invention provides a method of treating a subject afflicted with a substance use disorder (SUD) comprising administering to the subject an effective amount of a compound having the structure: wherein A is a ring structure, with or without substitution; X1 is C or N; X2 is N, O, or S; Y1 is H, -(alkyl), -(alkenyl), -(alkynyl), -(cycloalkyl), -(haloalkyl), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y2 is H, -(alkyl), -(alkenyl), -(alkynyl), -(cycloalkyl), -(haloalkyl), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y3 is H, -(alkyl), -(alkenyl), -(alkynyl), -(cycloalkyl), -(haloalkyl), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y4 is H, -(alkyl), -(alkenyl), -(alkynyl), -(cycloalkyl), -(haloalkyl), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y5 is H, -(alkyl), -(alkenyl), -(alkynyl), -(cycloalkyl), -(haloalkyl), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y6 is H, -(alkyl), -(alkenyl), -(alkynyl), -(cycloalkyl), -(haloalkyl), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); ? and ? are each pr

Abstract: The invention provides new heterocyclic compounds having the general formula (I) wherein A, L, X, m, n, R1 and R2 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.

Abstract: Described herein are KAT6A inhibitors and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of a disease or disorder associated with KAT6A.

Abstract: Described herein are macrocyclic compounds of Formula (I), which can inhibit kinases such as EGFR, including mutant forms such as T790M EGFR mutants. Also described herein are pharmaceutical compositions comprising a compound of Formula (I), or any pharmaceutically acceptable form thereof, processes for their preparation, and use in therapy for the prevention or treatment of cancer. In particular, compounds described herein can be effective for treating EGFR-driven cancers including non-small cell lung cancer (NSCLC).

Abstract: The present disclosure relates generally to compounds and compositions, and their use as kinase inhibitors.

Abstract: This disclosure provides modulators of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) having core structure (I), pharmaceutical compositions containing at least one such modulator, methods of treatment of CFTR mediated diseases, including cystic fibrosis, using such modulators and pharmaceutical compositions, combination pharmaceutical compositions and combination therapies employing those modulators, and processes and intermediates for making such modulators.

Abstract: The present disclosure provides a novel compound represented by the following Chemical Formula 1 and an organic light emitting device including the same: wherein R1 to R8 are described herein.

Abstract: Tri-component multi-functional boronated complexes (B-complexes), featuring reversible covalent bonds, are described, which incorporate a drug; a water-soluble moiety (e.g. polyethylene glycol (PEG) chains, cyclodextrins); and a targeting unit. A B-complex core was assembled in one step, and proved to be stable in different biocompatible conditions, such as human plasma, though reversible for example in the presence of glutathione (GSH). This platform enabled the modular construction of the multifunctional conjugates exhibiting high selectivity towards, for example, folate-receptor-positive MDA-MB-231 cancer cells, having an IC50 in the low nanomolar range.

Abstract: Silane precursors and related methods are provided. A method for preparing a silane precursor may comprise one or more of the following steps: contacting a dihalide silane compound and an amine in a first solvent to obtain a first reaction product; and contacting the first reaction product and a reductant in a second solvent to obtain a second reaction product.

Abstract: A pharmaceutically acceptable salt of an acyclic nucleotide phosphoramidate to treat HPV and related conditions including neoplasia, as well as pharmaceutical compositions, morphic forms and dosage forms thereof.