Abstract: The present invention relates to novel oxadiazoles of Formula I. wherein, R1, L1, A, L2 and R10 are as defined in the detailed description.

Abstract: The present invention relates to a compound exhibiting STAT3 inhibitory activity, or a pharmaceutically acceptable salt, solvate or hydrate of the same, and pharmaceutical uses of these. The compounds of the present invention efficiently inhibit the abnormal activity of STAT3 associated with various diseases and thus can be usefully utilized for the prevention and treatment of various STAT3-related diseases associated with cancer, autoimmune diseases, inflammatory diseases and the like.

Abstract: Provided herein are methods of making a thiazoline anti-hyperalgesic, Compound 1, and polymorphs thereof. The methods described herein use inexpensive reagents and are capable of providing Compound 1 in commercial-scale quantities. Also provided are pharmaceutical compositions of Compound 1 suitable for human administration.

Abstract: A method for preparing sugar-based mono and diesters is described. The process entails the esterification of 2,5-furan-dicarboxylic acid (FDCA) with an alcohol in the presence of low loadings of a homogeneous organotin (IV) catalyst.

Abstract: Disclosed is a process to produce a purified vapor comprising dialkyl-furan-2,5-dicarboxylate (DAFD). Furan-2,5-dicarboxylic acid (FDCA) and an alcohol in an esterification zone to generate a crude diester stream containing dialkyl furan dicarboxylate (DAFD), unreacted alcohol, 5-(alkoxycarbonyl) furan-2-carboxylic acid (ACFC), and alkyl furan-2-carboxylate (AFC). The esterification zone comprises at least one reactor that has been previously used in an DMT process.

Abstract: Disclosed are derivatives of icariin. Disclosed are compounds having Formula I-VIII as defined herein. Methods of using these compounds for the treatment of cancer and inflammation are also disclosed.

Abstract: The present invention relates to a method for producing a 1,3-dioxolane compound represented by formula 1, the method containing step (a), in which hexafluoroacetone monohydrate is brought into contact with a metal fluoride, step (b), in which fluorine gas is brought into contact, and step (c), in which an olefin compound represented by formula 2 is brought into contact. In formulae 1 and 2, X1 to X4 each independently represent a hydrogen atom, fluorine atom, chlorine atom, or trifluoromethyl group.

Abstract: Object of the invention is a process for the manufacturing of a polymer with urethane groups, wherein in a first alternative A) a five-membered cyclic monothiocarbonate B) a compound with at least two amino groups, selected from primary or secondary amino groups, and C) a compound which at least two functional groups that react with a group —SH or, in case of a carbon-carbon triple bond as functional group that react with a group —SH, a compound with at least one carbon-carbon triple bond are reacted or wherein in a second alternative A) a five-membered cyclic monothiocarbonate and D) a compound with at least one primary or secondary amino group and at least one functional group that reacts with a group —SH.

Abstract: Disclosed are processes and intermediates for the preparation of compound (X), which is currently being investigated for the treatment of prostate cancer.

Abstract: Described herein are amorphous and crystalline forms of the androgen receptor modulator 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide. Also described are pharmaceutical compositions suitable for administration to a mammal that include the androgen receptor modulator, and methods of using the androgen receptor modulator, alone and in combination with other compounds, for treating diseases or conditions that are associated with androgen receptor activity.

Abstract: This invention is based on the discovery that many lung diseases associated with aging are mediated at least in part by cells bearing a senescent phenotype. Senescent cells accumulate with age, and express factors that contribute to the pathophysiology of age related conditions. The severity of age-related conditions typically correlates with the abundance of senescent cells: thus, clearing senescent cells can help abrogate the condition: providing symptomatic relief, and potentially inhibiting disease progression. In accordance with this invention, a family of Bcl protein inhibitors has been developed for the treatment of lung diseases. These senolytic agents have an appropriate dose and specificity profile to be effective in the clinical management of previously intractable pulmonary diseases.

Abstract: The present invention relates to crystalline forms of ethyl 2-[[3-[[3-chloro-5-fluoro-6-[3-methyl-2,6-dioxo-4-(trifluoromethyl)pyrimidin-1-yl]-2-pyridyl]oxy]-2-pyridyl]oxy]acetate, herein after also referred to as “compound of formula (I)”.

Abstract: Described herein are compounds that are useful in treating a TYK2-mediated disorder. In some embodiments, the TYK2-mediated disorder is an autoimmune disorder, an inflammatory disorder, a proliferative disorder, an endocrine disorder, a neurological disorder, or a disorder associated with transplantation.

Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1 or a salt thereof, wherein q, r, s, Q, R1, R2?, R2?, R3 and R4 are as defined herein.

Abstract: The present invention provides pyrazole derivatives of Formula (I), and in particular N1-(4-(5-(cyclopropylmethyl)-1-methyl-1H-pyrazol-4-yl) pyridin-2-yl)cyclohexane-1,4-diamine derivatives and related compounds as casein kinase 1 (CK1) and/or interleukin 1 receptor associated kinase 1 (IRAKI) inhibitors for treating cancer, inflammatory and immune related disorders.

Abstract: The present invention relates to sulfonylureas and sulfonylthioureas comprising a 5-membered heteroaryl group substituted with a monovalent heteroaryl-containing group. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

Abstract: Provided are a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, ether, ester, prodrug and solvate thereof. The compound can be used for preventing and/or treating cancers.

Abstract: The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of HER2 or EGFR for the treatment or prevention of disease, including cancer.

Abstract: Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.

Abstract: Disclosed herein are compounds of Formula I: TL-La-CE-HD??(I) or a pharmaceutically acceptable salt, prodrug, amide or ester thereof, where i) TL is a moiety of Formula IIa, IIb, IIIa, IIIb, IIIc, or IIId; ii) CE is a moiety of Formula IV; iii) HD is a moiety of Formula V or VI; where the substituents are as defined herein. Disclosed are also pharmaceutical compositions comprising the above compounds, and methods of treating disease by administering or contact a patient with one or more of the above compounds.

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

Abstract: Disclosed are a compound with anthrone and N-containing heterocycle and an application thereof in an OLED. The compound contains anthrone and N-containing heterocycle structure which are both strong electron-withdrawing groups. The compound has a deep HOMO energy level and high electron mobility and is suitable for use as hole blocking materials or electron transport materials; the compound can also be used as a host material for electron-type light-emitting layers; in addition, the compound of the present invention has strong group rigidity, not easily causes crystallization and aggregation between molecules, and has good film-forming property. After the compound of the present invention is applied to an OLED device as an organic electroluminescent functional layer material, the current efficiency, power efficiency and external quantum efficiency of the device are greatly improved; moreover, the compound can improve the service life of the device.

Abstract: Provided herein are semisynthetic aurones, pharmaceutical compositions, and methods of treating cancer. The semisynthetic aurone compound including a structure according to Formula (I) or pharmaceutically acceptable salt thereof, where R1 is H, an alkyl cyano, an alkyl phenyl substituted with one or more halogens, or any combination thereof, and R2 is an aromatic group, a heterocycle, or a combination thereof. The pharmaceutical composition includes the semisynthetic aurone compound and a carrier. The method includes administering to a patient in need of such treatment an effective amount of the semisynthetic aurone compound.

Abstract: A benzofuran derivative, a preparation method thereof and a use thereof in medicine are described. In particular, a benzofuran derivative as shown by general formula (I), the preparation method thereof, a pharmaceutical composition containing the derivative, and uses thereof as an EZH2 inhibitor and in the prevention and/or treatment of diseases such as tumours and cancers, etc., and in particular, uses thereof in the prevention and/or treatment of non-Hodgkin's lymphoma, diffuse large B-cell lymphoma, follicular lymphoma and synovial sarcoma, are described.

Abstract: This invention relates to compounds of Formula (I) or a pharmaceutically acceptable salt thereof, in which R-groups R1 to R23, A, Q, U, V, W, X, Y, Z, n, p and q are as defined herein, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer, in a subject.

Abstract: Provided are compounds that enhance the efficacy of viruses by increasing spread of the virus in cells, increasing the titer of virus in cells, or increasing the antigen expression from a virus, gene or trans-gene expression from a virus, or virus protein expression in cells. Other uses, compositions and methods of using same are also provided.

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

Abstract: The present disclosure relates to indole compounds and pharmaceutical compositions thereof, and their use in stimulating the immune system of patients in need thereof and in treating cancer.

Abstract: This invention is directed to benzenesulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of diseases or conditions associated with voltage-gated sodium channels, such as epilepsy.

Abstract: Provided herein are small molecule agonists of the apelin receptor for the treatment of disease. The compounds disclosed herein are useful for the treatment of a range of cardiovascular, renal and metabolic conditions. The present invention is based on the seminal discovery of a series of potent small molecule agonists of the apelin receptor, which are useful for the treatment of diseases including heart failure, chronic kidney disease, hypertension, and metabolic disorders such as insulin resistance/diabetes and obesity. The compounds disclosed herein are highly specific for the apelin receptor versus the angiotensin II receptor (ATI).

Abstract: Methods of detecting a non-explosive analyte can include exposing a sensor compound to a non-explosive analyte and displaying a change in the sensor compound upon exposure of the sensor compound to the non-explosive analyte. A variety of sensor compounds for detecting a target analyte, including both explosive and non-explosive analytes, is also described. Sensor devices for detecting a target analyte can include a substrate and a sensor compound positioned on the substrate in a plurality of detection zones.

Abstract: Described herein are methods and compositions for the treatment of conditions, diseases, or disorders associated with autotaxin activity. The methods and compositions disclosed herein include the use of at least one autotaxin inhibitor compound.

Abstract: The present invention provides a compound having TrkA inhibitory activity, or a pharmaceutically acceptable salt thereof. The present invention relates to a compound represented by Formula (I): wherein ?X is ?O or the like, R5 and R5A are hydrogen atoms or the like, -A- is —NR1— or the like, B is substituted or unsubstituted aromatic carbocyclyl or the like, R1 is substituted or unsubstituted alkyl or the like, R2 is a hydrogen atom or the like, —W— is —CH2— or the like, —WA— is —CH2— or the like, R13 is substituted or unsubstituted aromatic carbocyclyl or the like, R14 is substituted or unsubstituted aromatic heterocyclyl or the like, R15 is substituted or unsubstituted alkyl or the like, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same.

Abstract: Disclosed are small molecule inhibitors of ?v?6 integrin, and methods of using them to treat a number of diseases and conditions.

Abstract: The present disclosure relates to novel hydroxyl or halogen substituted derivatives of C11-C22 alkanoic acid ester of Paliperidone compound of formula (formula II) and process for preparing the same. The said compounds used in pharmaceutical composition for the treatment of schizophrenia and schizoaffective disorder, wherein, R=C10-C21 alkyl substituted by hydroxy or halogen.

Abstract: The present invention provides solid state forms of Venetoclax, particularly relates to novel alkali metal salt and/or DMF solvate form of Venetoclax or its salt. The present invention also relates to process for the preparation Venetoclax by using the said solid state form of Venetoclax.

Abstract: The invention provides the tris salt of 4-(4-(1-isopropyl-7-oxo-1,4,6,7-tetrahydrospiro[indazole-5,4?-piperidine]-1?-carbonyl)-6-methoxypyridin-2-yl)benzoic acid as a crystalline anhydrous or tri-hydrate; as well as polymorphs, pharmaceutical compositions, dosage forms, and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase (ACC) enzyme(s) in an animal.

Abstract: The present invention provides novel crystalline forms B1 & B2 of linagliptin intermediate of structural formula V and methods for production of novel crystalline form of linagliptin intermediate represented by the following structural formula V.

Abstract: Compound of formula (I) and its addition salts with pharmaceutically acceptable acids, and methods in which an effective amount of the compound or any pharmaceutically acceptable salt thereof is administered (as a medicament) to an individual in need thereof.

Abstract: Described herein are compounds that may selectively bind to Hsp90, methods of using the compounds, and kits including the compounds. The compounds may allow for selective detection of Hsp90 in a sample.

Abstract: The present invention relates to a bicyclic nucleocapsid inhibitor and the use of the same as a drug in the treatment of hepatitis B. In particular, disclosed is a compound having the structure as shown in chemical formula A, or a stereoisomer or a tautomer thereof, or a pharmaceutically acceptable salt, a hydrate or a solvate thereof that can be used as an HBV inhibitor, wherein the definition of each group is as described in detail in the description. The present invention also relates to a pharmaceutical composition comprising the compound and the use of the same in the treatment of hepatitis B.

Abstract: The present invention provides novel compounds, compositions and methods for treating or preventing an IRE1?-related disease or disorder. In certain embodiments, the disease or disorder is selected from the group consisting of a neurodegenerative disease, a demyelinating disease, cancer, an eye disease, a fibrotic disease, and diabetes.

Abstract: The present invention relates to a method for preparing the compound of formula IV, compound of formula XI, and acalabrutinib, a new generation of bruton tyrosine kinase (BTK) inhibitor.

Abstract: A method of synthesizing comprising a step of making an imidazo-pyrimidine compound by coupling a first compound of formula (II) with a second compound of formula (III) Followed by a deprotection and tosylation step. The methods are able to produce an isotopically substituted molecule having upwards of 95% purity relative to non-isotopically substituted molecules.

Abstract: The present invention provides a compound of Formula I: wherein R is hydrogen or methyl; and Z is: or a pharmaceutically acceptable salt thereof, and the use of compounds of Formula I for treating neurodegenerative diseases, such as Alzheimer's disease.

Abstract: The present invention relates to a bromodomain inhibitor. Provided are a compound represented by general formula I or a pharmaceutically acceptable salt, enantiomer, diastereomer, atropisomer, racemate, polymorph, solvate, or isotopically labeled compound (including deuterium substitution) thereof, a preparation method of the same, a pharmaceutical composition comprising the same, and a pharmaceutical use thereof.

Abstract: The invention relates to 1,2,3?,5?-tetrahydro-2?H-spiro[indole-3,1?-pyrrolo[3,4-c]pyrrole]-2,3?-dione compounds 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 cancer, immune diseases, inflammatory conditions, allergic skin diseases associated with excessive proliferation, blinding disease and viral infections.

Abstract: Herein is described the design and synthesis of resorcylate aminopyrazole compounds. These compounds show broad, potent and fungal-selective Hsp90 inhibitory activity. These compounds also find use in treating Hsp90 related diseases.

Abstract: Disclosed herein are chemical entities, or pharmaceutically acceptable salts thereof, for treating fibrosis, including pulmonary fibrosis, such as idiopathic pulmonary fibrosis. Also disclosed herein are pharmaceutical formulations for treating fibrosis, the pharmaceutical formulations including one or more of the foregoing chemical entities and one or more pharmaceutically acceptable excipients, carriers, vehicles, or a combination thereof. Also disclosed herein are packaged pharmaceutical formulations for treating fibrosis, the packaged pharmaceutical formulations including one of the foregoing pharmaceutical formulations and instructions for using the pharmaceutical formulation to treat a patient having fibrosis or susceptible to fibrosis. Also disclosed herein is a method for treating fibrosis, the method including administering one of the foregoing pharmaceutical formulations.

Abstract: The invention relates to quinoxaline derivatives of the general formula I, and the use of the compounds of the present invention for the treatment and/or prevention of hyperproliferative or infectious diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.