Abstract: The invention relates to novel cell-binding agent-maytansinoid conjugate having a self-immolative peptide linker and more specifically to conjugates of formula (I). The invention also provides novel maytansinoid compounds of formula (II), (III), (IV) or (V). The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.

Abstract: The present invention relates to a method for producing N-substituted sulfonamide compounds including a step of reacting a sulfonamide compound of general formula (1) with a halogenated organic compound of general formula (2) in the presence of cesium carbonate or potassium carbonate in an organic solvent to produce an N-substituted sulfonamide compound of general formula (3).

Abstract: The present invention relates to a compound represented by formula I and a non-toxic pharmaceutically acceptable salt thereof. In formula (I), R1 is H, CH3 or deuterated methyl (CD3); R2 is CH3 or CH2CH3; R3, R4 and R5 are each independently H or deuterium (D); when R1 is H or CH3, at least one of R3, R4 and R5 is D.

Abstract: The present compositions and methods generally relate to the treatment of diseases, such as idiopathic pulmonary fibrosis (IPF) and neurodegenerative diseases related to tau aggregation.

Abstract: Disclosed herein are methods and materials for improving brain function and/or promoting neurogenesis m a patient suffering from impaired brain function. Specifically exemplified herein ls the co-administration of phenserine and NBI-18. A method of treating a neurodegenerative disease in a patient in need thereof, said method comprising co-administering to the patient phenserine, or pharmaceutically acceptable salt thereof, and NBI-18, or pharmaceutically acceptable salt thereof, in respective amounts and frequency such that they work together to improve brain function or induce neurogenesis in the patient.

Abstract: The present disclosure relates to certain macrocyclic derivatives, pharmaceutical compositions containing them, and methods of using them to treat disease, such as cancer.

Abstract: Provided herein are supramolecular assemblies, the supramolecular assemblies comprising a racemic mixture of rigid macrocycles capable of interacting through [C—H . . . O] hydrogen bonds. Also provided herein are methods for preparing supramolecular assemblies, the method comprising providing a mixture of rigid macrocycles capable of interacting through [C—H . . . O] hydrogen bonds, the mixture of rigid macrocycles comprising a first rigid macrocycle enantiomer and a second rigid macrocycle enantiomer, and providing a solvent.

Abstract: Described herein are compositions and methods for use in targeted drug delivery using cell-surface receptor binding drug delivery conjugates containing hydrophilic spacer linkers for use in treating disease states caused by pathogenic cell populations.

Abstract: Disclosed are compounds of Formula (I) to (IV): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate or prodrug thereof. Also disclosed are methods of using such compounds as PAR4 inhibitors, and pharmaceutical compositions comprising such compounds. These compounds are useful in inhibiting or preventing platelet aggregation, and are useful for the treatment of a thromboembolic disorder or the primary prophylaxis of a thromboembolic disorder.

Abstract: Water soluble fluorogenic sensors for detecting a hydrazine analyte are provided. Aspects of the fluorogenic sensors include at least one water soluble group and a hydrazine reactive group. Methods of evaluating a sample for the presence of a hydrazine analyte and methods of detecting hydrazine diffusion across a phospholipid membrane are provided. Kits for practicing the subject methods are also provided.

Abstract: The invention relates to new heteroaryl derivatives of the formula wherein X is selected from the group consisting of: N and CH; X is selected from the group consisting of: N and CF; (with the proviso that at least one of X1 and X2 is N), and A is as defined in the description and claims, to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: Pharmaceutical and chemical intermediates and related chemistry providing a green preparation method for quinoline compounds. N-Substituted arylamine derivatives as raw material react with arylacetylene or arylethylene derivatives for 24 hours at 80° C.-160° C. in the presence of Brønsted acid catalyst and oxidant without solvent, to obtain quinoline compounds. Beneficial characteristics include convenient operation, mild reaction conditions, environmentally friendly property and possibility of realizing industrialization, and provides the quinoline compounds in high yields. The quinoline compounds synthesized by this method can be further functionalized into various compounds which have potential applications in development and research of natural products, functional materials and fine chemicals.

Abstract: This disclosure relates bis-amine compounds disclosed herein and uses related to CXCR4 inhibition. In certain embodiments, the compounds have formula (I), salts, derivatives, and prodrugs thereof wherein, A is a bridging aryl or heterocyclyl and R1 and R2 are further disclosed herein. In certain embodiments, the disclosure contemplates pharmaceutical compositions comprising compounds disclosed herein. In certain embodiments, the disclosure relates to methods of treating or preventing CXCR4 related diseases or conditions by administering an effective amount of a compound disclosed herein to a subject in need thereof.

Abstract: The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl, and pyrrolo[2,3-b]pyridinyl acrylamides, epoxides, and analogues thereof. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.

Abstract: A method for preparing chromium(III) pyridine-2-carboxylate using 2-OP rectification residues, including: subjecting the 2-OP rectification residues to in-situ catalytic pyrolysis and vacuum distillation, room-temperature crystallization and separation, recrystallization and dehydration, alkali-catalyzed hydrolysis, acidification and complexation, and separation, washing and drying to prepare a chromium(III) pyridine-2-carboxylate product, of which a yield is greater than 50% of the weight of the 2-OP rectification residues. The acidification and complexation includes: cooling the aqueous solution containing sodium pyridine-2-carboxylate obtained from the alkali-catalyzed hydrolysis to a temperature below 50° C.; adjusting the aqueous solution to pH 3.0-8.5 with 5-50 wt % dilute H2SO4 or 3-30 wt % dilute HCl followed by batchwise addition of CrCl3, Cr(NO3)3 or Cr2(SO4)3 for complexation at 20-70° C.

Abstract: The present invention relates to cyclic amino acid molecules, in particular 1,3,4-oxadiazole containing macrocyclic peptides, and a process to produce the same. The process involves the macrocyclization of amino acids or linear peptides. Specifically, the process comprises reacting an amino acid molecule with an isocyano-iminophosphorane and an aldehyde or a ketone.

Abstract: In one aspect, the present disclosure provides caffeic acid derivatives of the formula: wherein the variables are as defined herein. In another aspect, the present disclosure provides pharmaceutical compositions and methods of using of the compounds disclosed herein, including for the treatment of cancer.

Abstract: Disclosed is a purified dialkyl furan dicarboxylate (DAFD) vapor composition containing at least 99.5 wt. % DAFD; 5-(alkoxycarbonyl) furan-2-carboxylic acid (ACFC) that, if present, is present in an amount of not more than 1000 ppm, alkyl-5-formylfuran-2-carboxylate (AFFC) that, if present, is present in an amount of not more than 1000 ppm, 5-(dialkoxymethyl)furan-2-carboxylic acid (DAFCA) that if present, is present in an amount of not more than 1000 ppm, and alkyl 5-(dialkoxymethyl)furan-2-carboxylate (ADAFC) that if present, is present in an amount of not more than 1000 ppm, in each case based on the weight of the DAFD vapor composition.

Abstract: A new process for the preparation of fexofenadine and of related intermediates, which can be used in the preparation of fexofenadine, is provided.