Abstract: Provided herein are methods for treating, preventing, or ameliorating one or more symptoms of a condition, disorder, or disease mediated by a lipid kinase or a protein kinase with benzimidazoles, for example, of Formula I or II, and pharmaceutical compositions thereof. Also provided herein are benzimidazoles, and pharmaceutical compositions thereof; and methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.

Abstract: The invention provides compounds of formula I, wherein the substituents are as set out in further detail in the specification. The compounds are potent inhibitors of GCN2 and they have excellent pharmacokinetic properties. The compounds are useful for the treatment or prevention of a variety of conditions, particularly cancer. The invention further provides pharmaceutical compositions comprising the compounds of the invention and uses of the compounds and the compositions.

Abstract: The present disclosure provides a compound of Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein Rx and X1 are as defined herein, and methods of making and using same.

Abstract: This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.

Abstract: Provided are a compound of formula (I) or a tautomer, a mesomer, a raceme, an enantiomer, a diastereoisomer, or a pharmaceutically acceptable salt thereof, and the use thereof in the preparation of drugs for diseases mediated by CDK9.

Abstract: Provided are 5-oxo-4,5-dihydro-1H-1,2,4-triazole compounds, which are the inhibitors of dihydroorotate dehydrogenase (DHODH). More specifically, provided are the preparation of the compounds and their use in the preparation of pharmaceutical composition for the treatment of various diseases, conditions and disorders related to DHODH activity.

Abstract: The present disclosure relates to compounds comprising a VHL ligand moiety and to methods of using such compounds as ligands of VHL. The present disclosure further relates to the use of the compounds described herein, or pharmaceutical compositions thereof, to prevent and/or treat a range of diseases, disorders, and conditions.

Abstract: The disclosure provides at least one entity chosen from compounds of formula (I), solid state forms of the same, compositions comprising the same, and methods of using the same, including use in treating focal segmental glomerulosclerosis (FSGS) and/or non-diabetic kidney disease (NDKD).

Abstract: The invention relates to an improved process for synthesizing 6-(cyclopropaneamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)amino)-5N-(methyl-d3)pyridazine-3-carboxamide of the formula: Compound I is currently in clinical trials for the treatment of auto-immune and auto-inflammatory diseases such as psoriasis.

Abstract: Disclosed are a crystal form and a pharmaceutically acceptable salt of a ketohexokinase inhibitor, a preparation method therefor, and a pharmaceutical composition and use thereof, which specifically relate to a crystal form of a compound of formula (1), a pharmaceutically acceptable salt of the compound of formula (1), and a crystal form of the pharmaceutically acceptable saltserving as the KHK inhibitor, a preparation method therefor, a pharmaceutical composition containing the crystal form, the pharmaceutically acceptable salt, and the crystal form of the pharmaceutically acceptable salt, and use of the crystal form and the pharmaceutically acceptable salt of the compound of formula (1), and the crystal form of the pharmaceutically acceptable salt in the preparation of a medicament for treatment and/or prevention of a KHK-mediated disease or related disease.

Abstract: The use of tocotrienols in medicine, veterinary or cosmetics, namely through the stabilization of tocotrienols, in particular in cosmetic formulations without hampering its functions in the skin is provided. In particular, the modification of tocotrienols with nicotinic acid results in the stabilization of the molecule and the penetration profile in human skin. The compounds and composition of are useful in medicine, veterinary or cosmetic industry namely in the prevention, therapy or treatment of skin diseases, skin disorders, or as a therapy or treatment of acne, seborrheic dermatitis or as an anti-aging agent.

Abstract: The present application describes GLP-IR modulating compounds that are useful for treating GLP-IR-mediated diseases or conditions.

Abstract: Here we report the discovery of 2-(4-(3-(trifluoromethoxy)phenoxy)picolinamido)benzo[d]oxazole-5-carboxylate as an antibacterial with potent and selective activity against C. difficile. Its MIC50 and MIC90 values, documented across 101 strains of C. difficile, are 0.12 and 0.25 ?g/mL, respectively. The compound is effective against C. difficile both at the logarithmic (vegetative) and stationary phases of growth. It targets cell-wall biosynthesis, as assessed both by macromolecular biosynthesis assays and by scanning-electron microscopy. Animals infected with a lethal dose of C. difficile and treated with compound 1 had better survival compared to treatment with vancomycin, which is the front-line antibiotic used for severe recurrent C. difficile infection.

Abstract: A series of substituted 4,4-difluorocyclohexyl 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: Disclosed are compounds of following formula (I): in which all symbols have the same meanings as the definitions described in the specification; or a salt thereof. The compounds or a salt thereof are useful as a prophylactic and/or therapeutic agent for cancer, Huntington's disease, Alzheimer's disease and the like.

Abstract: The present invention relates to compounds that act as DUX4 repressors, suitable for the treatment of diseases related to DUX4 expression, such as muscular dystrophies. It also relates to use of such compounds, or to methods of use of such compounds.

Abstract: Compounds are provided having structure (I): or a pharmaceutically acceptable salt, solvate, hydrate, isomer, or isotope thereof, wherein X, L, Y, R1, R2, R3 and Cy are as defined herein. Pharmaceutical compositions containing such compounds, as well as the compounds themselves, are also provided. Methods are provided wherein the compounds are inhibitors of one or both of diacylglycerol kinase alpha (DGK?) and diacylglycerol kinase zeta (DGK?) or are useful in the treatment of diseases, disorders and conditions related to DGK? and/or DGK? activity. More specifically, methods of treating a proliferative or a viral infection are provided by administering to a subject in need thereof, an effective amount of the pharmaceutical composition containing compounds of structure (I).

Abstract: The present invention relates to a novel compound having a histone deacetylase 6 (HDAC6) inhibitory activity, an isomer thereof or a pharmaceutically acceptable salt thereof, the use thereof for preparing a therapeutic medicament; a pharmaceutical composition containing the same, and a treatment method using the composition; and a preparation method thereof. The novel compound, the isomer thereof, or the pharmaceutically acceptable salt thereof according to the present invention has the HDAC6 inhibitory activity, which is effective in the prevention or treatment of HDAC6-mediated diseases including cancer, inflammatory diseases, autoimmune diseases, neurological or neurodegenerative diseases.

Abstract: Substituted amide derivatives are useful for the prevention and/or treatment of several medical conditions including hyperproliferative disorders and diseases.

Abstract: The present disclosure provides compounds of formula (I) and methods useful for inhibiting SARM1 and/or treating and/or preventing axonal degeneration.

Abstract: A salt and crystal form of a dihydropyrido[2,3-d]pyrimidine derivate, and specifically, a crystal form of a fumarate hydrate of compound 1, and a preparation method thereof are provided. In the formula, X is 2.0-3.0. The X-ray powder diffraction pattern expressed in 2? angles using Cu-Ka radiation has characteristic peaks at 2? values of 9.28°±0.2° and 3.63°±0.2°. The crystal form has good stability and can better be applied to clinical practice.

Abstract: The present invention relates to a compound, a pharmaceutical composition containing thereof, preparation methods therefor, and use thereof as BCL-2 inhibitors. The compound is a compound represented by formula (I), or an isomer, prodrug, solvate, stable isotopic derivative or pharmaceutically acceptable salt thereof. The invention also relates to use of the compound for treating or preventing diseases mediated by BCL-2, such as tumors, and to a method for using the same for treating described diseases.

Abstract: The invention relates to compounds of formula (A) and formula (I): or a salt thereof, wherein R1, R2, R10, R11, R12, R13, R14, R15, R16, q and p are as described herein. Compounds of formula (A), formula (I), and pharmaceutical compositions thereof are ?v?6 integrin inhibitors that are useful for treating fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).

Abstract: This disclsore relates to compounds according to Formula (I), salts, prodrugs and pharmaceutical formulation comprising the compound are provided herein for the treatment of CXCR4 and CCR5 related conditions. The conditions may include viral infections, abnormal cellular proliferation, retinal degeneration and inflammatory diseases, or the compounds may be used as immunostimulants or immunosuppressants. Furthermore, the compounds may be used in combination with another active ingredient selected from an antiviral agent or chemotherapeutic agent.

Abstract: The invention relates to pharmaceutical compositions comprising 4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-1-(4-fluorophenyl)-butan-1-ol, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) pathway and/or the dopamine D2 receptor pathway, and methods of treating conditions of the central nervous system therewith.

Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: or a pharmaceutically acceptable salt, wherein the variables are as devined herein. Moreover, The compounds of this invention have formula I-A: or a pharmaceutically acceptable salt, wherein the variables are as defined herein.

Abstract: Described herein are triazalone compounds of Formula (I) and pharmaceutically acceptable salts thereof. Methods of making and using compounds of Formula (I) are also described. Compounds of Formula (I) and pharmaceutically acceptable salts thereof can be useful as adenosine receptor antagonists, for example in the treatment of diseases or conditions mediated by the adenosine receptor, such as cancer, movement disorders, or attention disorders.

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: This disclosure relates to compounds of formula (I) as defined in the Specification. This disclosure also relates to methods of synthesizing the compound of formula (I) and using the compounds of formula (I) for treating a disease (e.g., cancer).

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

Abstract: Disclosed is a compound of a general formula (I), which may be used for the treatment of ATR kinase-mediated diseases, for example, proliferative diseases such as cancer. Further disclosed are a preparation method for the compound of the general formula (I), a pharmaceutical composition, and use of the pharmaceutical composition for the treatment of ATR kinase-mediated diseases.

Abstract: A nitrogen-containing fused ring derivative inhibitor, a preparation method therefor and the use thereof. The present invention particularly relates to a compound as shown in general formula (I), a preparation method therefor, a pharmaceutical composition thereof, and the use thereof as an NK inhibitor in the treatment of depression, anxiety, schizophrenia, sex hormone-dependent diseases and other related diseases. The various substituents in general formula (I) have the same definition as that in the description.

Abstract: The present invention relates to the technical field of chemical drug synthesis, and specifically relates to a method for preparing a compound as shown in formula I, comprising: treating the compound as shown in formula VII with an acid to generate the compound as shown in formula I. The method has few synthetic process steps, raw materials which is stable and is easy to prepare, a reaction process which is easy to control, and a high overall yield and purity, and is suitable for industrial preparation.

Abstract: Crystalline Forms of Compound (I): pharmaceutically acceptable salts thereof and solvates of any of the foregoing are disclosed. Pharmaceutical compositions comprising the same, methods of treating disorders and conditions associated with oncogenic KIT and PDGFRA alterations using the same, and methods for making Compound (I) and crystalline forms thereof are also disclosed.

Abstract: The present disclosure relates to compounds of Formula (I?): and to their prodrugs, pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for modulating orexin receptor activity and may be used in the treatment of disorders in which orexin receptor activity is implicated, such as narcolepsy, a hypersomnia disorder, a neurodegenerative disorder, a symptom of a rare genetic disorder, a mental health disorder, a metabolic syndrome, osteoporosis, cardiac failure, coma, or a complication in emergence from anaesthesia.

Abstract: The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment(including treatment of rheumatoid arthritis and atopic dermatitis), kits, methods of synthesis, and products-by-process.

Abstract: Disclosed are compounds of formula I, II, III, and IV, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of ALK2 kinase. Also provided are pharmaceutical compositions comprising a compound of formula I, II, III, or IV, or pharmaceutically acceptable salt thereof, and methods involving use of the compounds or pharmaceutically acceptable salts thereof and compositions in the treatment and prevention of various diseases and conditions, such as fibrodysplasia ossificans progressiva.

Abstract: The present invention provides 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); Y 2 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); Y 4 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); a and P are each present or absent and when present each is a bond.

Abstract: The present disclosure relates to the biopharmaceutical field, in particular, Exatecan derivatives, linker-payloads, and conjugates and thereof antibody-drug conjugates, and the corresponding preparing process and use thereof.

Abstract: Described herein are crystalline forms of (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydropyrido [3,2-b][1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide, the process of preparing the forms, and pharmaceutical compositions methods of use thereof.

Abstract: The disclosure includes compounds of Formula (A): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12, j, k, m, n, Y, W, W1, W2, W3, V, L, Z1, Q1, Q2, Q3, and Q4, are defined herein. Also disclosed is a method for treating a neoplastic disease, an autoimmune disease, or a neorodegenerative disease with these compounds.

Abstract: Disclosed is a tricyclic pyrimidinone compound of Formula (I) or a pharmaceutically acceptable salt thereof, which is an entirely new Lp-PLA2 inhibitor useful in treating neurodegeneration-related diseases such as Alzheimer's disease (AD), glaucoma and age-related macular degeneration (AMD), or cardiovascular diseases including atherosclerosis.

Abstract: Provided herein are compounds that are useful intermediates that may used to synthesize myeloid cell leukemia 1 protein (Mcl-1) inhibitors. Also provided are Mcl-1 inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.

Abstract: The present invention relates to a codrug that cleaved in the gut, preparation therefor, and a use thereof. Specifically, provided is a codrug compound in formula I. Also provided are a method of using the present compound for the treatment of gastrointestinal tract autoimmune diseases, inflammatory diseases, and cancers, as well as a method and an intermediate for preparing the present compound.

Abstract: The present invention relates to functionalized isonitrile compounds, formed by means of multicomponent environmentally friendly reactions, suitable for coupling to functional molecules such as biomolecules, APIs, chromophore and fluorophore molecules. The invention also relates to conjugates between said isonitrile compounds and functional molecules, which are useful in the synthesis of pharmaceutic drugs or tools, fluorescent molecules and labels, polymeric smart materials. The invention furthermore provides a kit for the in-vitro preparation of the functionalized isontrile compounds and conjugates. The invention also contemplates the medical use of said compounds and conjugates.

Abstract: Borylated Amino Acid compositions comprising tyrosine derivatives BTS and BTS(OMe) and novel methods of making BTS and BTS(OMe) are disclosed herein. Consequently, the BTS and/or BTS(OMe) can be scaled up to commercial scale and administered to patients as a Neutron Capture Agent and provide a method of treating cancer, immunological disorders, and other disease by utilizing a Neutron Capture Therapy modality.

Abstract: A preparation method for glufosinate ammonium or a salt thereof, an enantiomer thereof, or mixtures of the enantiomer thereof in all ratios, comprising reacting a compound of formula (II) or a salt, an enantiomer, or mixtures of the enantiomer in all ratios with one or more compounds of formula (III) or mixtures thereof.

Abstract: Disclosed herein are a crystalline or amorphous form of a Bcl-2/Bcl-xL inhibitor compound or a salt thereof, and a preparation method and application thereof.

Abstract: Some embodiments relate to precursors (including intermediate precursors) and related methods. To prepare an intermediate precursor, a mixture of bis (arene) metal complexes is combined with a first arene. The mixture of bis (arene) metal complexes and the first arene are heated and subsequently cooled. Upon cooling, a bis (first arene) metal complex precipitates from solution to obtain an intermediate precursor with high purity. To prepare a precursor, the bis (first arene) metal complex is contacted with a second arene and heated to obtain a precursor with high purity.

Abstract: A method for producing an organometallic nucleophile includes reacting an organohalide and a metal or metal compound with each other by a mechanochemical process in the presence of an ether compound in an amount of 0.5 to 10.0 equivalents relative to 1 equivalent of the organohalide. By utilizing the method, a method for producing an organometallic nucleophile can be performed without using a large-scale apparatus, a reaction method for reactions between an organometallic nucleophile and various organic electrophiles can be performed by an efficient and simplified means, and a simplified method for producing an organometallic nucleophile can be performed with high reactivity.