Abstract: The invention relates to novel crystalline forms of imiquimod formed with ferulic acid, acetic acid, coumaric acid, citric acid, or tartaric acid, to methods of making these cocrystals, and to compositions containing the cocrystals.

Abstract: A compound of the formula (I) wherein R represents a straight or branched, primary or secondary acyclic hydrocarbyl C3-C15 group, which can be saturated or unsaturated, or a straight or branched, primary or secondary acyclic hydrocarbyl C3-C15 group, which can be saturated or unsaturated and wherein one or more of hydrogen atoms is replaced with fluorine atom; X represents hydrogen atom or halogen atom, and * denotes chiral center, and salts thereof. The compound is useful for the treatment of diseases mediated by GPR40, in particular type II diabetes.

Abstract: An object is to provide a method for easily producing maleimide (MI) in which trace amounts of residual acid components as impurities in a crude MI are efficiently reduced, that is, the acid value is sufficiently reduced. <1> A method for producing purified MI, comprising reducing an acid value of crude MI by 50% or more, by adding carbodiimide (CDI) to a solution comprising the crude MI to react an acid component in the crude MI with the CDI. <2> The method for producing purified MI, comprising adding 0.5% by mass or more and 8% by mass or less of the CDI with respect to a mass of the crude MI for reaction. <3> The method for producing purified MI, wherein the CDI is N,N?-diisopropyl carbodiimide (DIC). <4> The method for producing purified MI, comprising removing a urea derivative of the CDI (CDI-U) by-produced when reacting the acid component in the crude MI with the CDI.

Abstract: Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds that are useful for the treatment of retinal binding protein (RBP4) related diseases, such as macular degeneration and the like.

Abstract: Novel pyrido[3,4-b]indole-6-carboxylic acid compounds, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The pyrido[3,4-b]indole-6-carboxylic acid compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.

Abstract: The invention is directed to a process for the ring-opening of a cycloadduct obtainable from a reaction of a furanic compound and a diene, said process comprising contacting the cycloadduct with an acidic mixture comprising sulfuric acid and an activating agent to obtain a ring-opened product. The present invention is particularly directed a continuous process.

Abstract: The present invention relates to novel solid crystalline form of N-methyl-2-(4-methyl-1,4-diazepan-1-yl)benzo [4,5]imidazo[1,2-a][1,8]naphthyridine-6-carbaxomide, processes for the preparation thereof, compositions thereof and method of use thereof.

Abstract: The invention relates to compounds of formula (I) which are inhibitors of MKK4 (mitogen-activated protein kinase kinase 4) and their use in promoting liver regeneration or reducing or preventing hepatocyte death. The compounds selectively inhibit protein kinase MKK4 over protein kinases JNK and MKK7. (I), wherein Rx, Ry, Rz and Rzz are selected from: a) Rx and Ry are F and Rz and Rzz are H; b) Rx, Ry and Rzz are independently halogen and Rz is H; c) Rx Rz and Rzz are independently halogen and Ry is H; and d) Rx Ry and Rz are independently halogen and Rzz is H.

Abstract: The present disclosure relates to solid forms and salts, crystalline and otherwise, of (E)-2-[[3-(3-methoxy-4-propargyloxy)phenyl)-1-oxo-2-propenyl]amino]benzoic acid and pharmaceutical compositions comprising same. The use of such solid forms, salts, and pharmaceutical compositions, for treating, preventing, or ameliorating diseases or conditions associated with fibrosis, inflammation and/or proliferation are disclosed.

Abstract: Provided herein is a method of treating, preventing, or ameliorating one or more symptoms of an untreated or treatment-resistant diabetes with a glucokinase activator, optionally in combination with a dipeptidyl peptidase-4 inhibitor.

Abstract: A biphenyl compound represented by formula (I), a preparation method therefor and an application thereof. The present invention also relates to a pharmaceutical composition that comprises the compound as an active ingredient. The compound is a novel small molecule immunomodulator having excellent oral absorption features and can be used for treating and/or preventing various immunity-related diseases.

Abstract: Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a purified compound described herein.

Abstract: The present disclosure provides GLP-1R agonists, and compositions, methods, and kits thereof. Such compounds are generally useful for treating a GLP-1R mediated disease or condition in a human.

Abstract: A dialkyl carbonate is prepared by reacting urea with an alkyl monohydric alcohol at 70° C. to 150° C. under normal pressure or reduced pressure. The reaction is conducted for 6 h to 30 h under stirring and reflux, with one or more of magnesium, calcium, aluminum, chromium, manganese, iron, cobalt, nickel, copper and zinc as a primary catalyst and one or more compounds including an electron-donating nitrogen, phosphonis, oxygen or sulfur atom as a catalyst promoter. The dialkyl carbonate is prepared under low reaction temperature and normal pressure or reduced pressure, with high selectivity and high yield. With simple operations, high safety and low cost for the process, the method has prominent industrial application prospects.

Abstract: Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.

Abstract: Stable, injectable pharmaceutical compositions are provided, which are useful as ready-to-dilute (RTD) or ready-to-use (RTU) liquid injectable compositions comprising bendamustine or a pharmaceutically acceptable salt thereof, and which are suitable for intravenous administration. Preferably, solution formulations comprise (a) bendamustine, or pharmaceutically acceptable salts, solvates, or hydrates thereof, (b) at least one pharmaceutically acceptable non-aqueous solvent; (c) optionally, at least one pharmaceutically acceptable excipient, and (d) optionally, a pH adjuster, where the pharmaceutical composition is antioxidant-free, and formulated as a ready-to-dilute or ready-to-use liquid composition suitable for parenteral administration. The invention further relates to methods for manufacturing stable, antioxidant-free injectable solutions of bendamustine.

Abstract: Provided is an alkynyl(hetero)aromatic compound having an inhibitory effect to protein tyrosine kinase, a pharmaceutical composition comprising same, preparation and usage thereof. Specifically, disclosed is an alkynyl(hetero)aromatic compound as shown in formula (I), wherein rings A, R1, R2, R3, R4, R5, L, and B are defined in the description, a pharmaceutically acceptable salt, a stereoisomer, a solvate, a hydrate, a crystal form, a prodrug or an isotopic variant thereof. The compound can be used for treating and/or preventing protein tyrosine kinase-related diseases, such as anti-tumor.

Abstract: The present invention is directed to pyridine N-oxide derivatives, stereoisomers, isotopologues, isotopomers and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing said compounds and the use of said compounds in the treatment and/or prophylaxis of thromboembolic disorders, inflammatory disorders and diseases or conditions in which plasma kallikrein activity is implicated.

Abstract: The present disclosure relates to compounds of formula (I) and pharmaceutical compositions and their use in reducing Widely Interspaced Zinc Finger Motifs (WIZ) expression levels, or inducing fetal hemoglobin (HbF) expression, and in the treatment of inherited blood disorders (e.g., hemoglobinopathies, e.g., beta-hemoglobinopathies), such as sickle cell disease and beta-thalassemia.

Abstract: Disclosed herein are compounds of Formula I?: or a stereoisomer or a tautomer thereof, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising such compounds, and methods of treating disease by administering or contacting a subject with one or more of the above compounds.