Abstract: The present invention relates to a novel process for preparing a compound of formula (III) and rhenium chelated MAG3 oligonucleotides.

Abstract: Disclosed herein are substituted hexahydro-1H-cyclopenta[c]pyrrole compounds, which may be useful as antagonists of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating disorders using the compounds and compositions.

Abstract: The disclosure discloses a method for synthesizing N-substituted phenyl-5-hydroxymethyl-2-oxazolidinone, wherein the method comprises: reacting from raw materials, 3-R2-4-R1-aniline and epichlorohydrin, and allowing the resulting product to react under alkaline conditions in a CO2 atmosphere to obtain N-substituted phenyl-5-hydroxymethyl-2-oxazolidinone, wherein R1 is a morpholine group, a morpholin-3-one group or a piperazine group, and derivative groups thereof, and R2 is halogen, hydrogen or lower alkyl. The method provided by the disclosure has such advantages as few steps, simple operation, cheap and easily available raw materials, mild reaction conditions, and high product yield, and is especially suitable for industrial production of antibiotic linezolid intermediates and antithrombotic drug rivaroxaban intermediates.

Abstract: Provided herein are topical formulations including a compound of formula (I) and methods of using these topical formulations for the treatment of skin diseases, wherein the topical formulations include non-aqueous gel, aqueous gel, and emulsion-based formulations; and the compound of formula (I) is represented by wherein R1, R2, R2a, R3, R3a, and R3b are as defined and described herein.

Abstract: The application is directed to compounds of formula (I): and pharmaceutically acceptable salts, radiolabeled isomers, solvates, or hydrates thereof, wherein R1, R2, R3, X, and n are defined as set forth in the specification. The application is also directed to compounds of formulae II, I-a, I-a1, I-a2, I-b, and I-b1 and the pharmaceutically acceptable salts, radiolabeled isomers, solvates, and hydrates thereof. The application is also directed to use of Compounds of the present disclosure to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain Compounds of the present disclosure are especially useful for treating pain. In one embodiment, Compounds of the present disclosure exhibit less opioid-induced side effects (such as, euphoria or drug-liking).

Abstract: The invention provides compositions and methods for epidural administration of the compound MCOPPB or a pharmaceutically acceptable salt thereof for treating pain, such as nociceptive pain suffered by an adult human.

Abstract: The present disclosure provides methods for inhibiting entry of a virus into a host cell using picolinic acid or a salt or derivative thereof. The present disclosure also provides methods for treating or preventing a viral infection in a subject by administering picolinic acid or a salt or derivative thereof. In particular, the methods of the present disclosure are effective for enveloped viruses and syncytium-forming viruses. In some embodiments, the present disclosure provides methods of treating or preventing a SARS CoV-2, Influenza A virus, human parainfluenza virus, herpes simplex virus, Japanese encephalitis virus, Zika virus, or a flavivirus infection.

Abstract: Provided herein are modified amino acids comprising an azido group, polypeptides, antibodies and conjugates comprising the modified amino acids, and methods of producing the polypeptides, antibodies and conjugates comprising the modified amino acids. The polypeptides, antibodies and conjugates are useful in methods of treatment and prevention, methods of detection and methods of diagnosis.

Abstract: There is provided tinostamustine or a pharmaceutically acceptable salt thereof for use in the treatment of sarcomain a patient in need thereof.

Abstract: Method for the production of formula (I) lumateperone or its acid addition salts so that the enantiomer compound with stereochemistry 6bR,10aS is separated form the cis racemate using resolution and the formula (II) stereoisomer is alkylated with 4-halo-4?-fluoro butyrophenone (X=I, Br, Cl) to produce the formula (I) lumateperone, or optionally its acid addition salt. The object of the invention also relates to the amorphous form of the morphologically uniform p-toluenesulfonic acid salt of lumateperone and to the naphthalene-2-sulfonic acid salt of lumateperone, to the 1:2 stoichiometry salt of lumateperone formed with naphthalene-2-sulfonic acid.

Abstract: Provided are methods of treating an injury to the nervous system in a subject comprising administering to the subject an effective amount of boldine, a boldine analog, or a pharmaceutically-acceptable salt thereof. Also provided are methods of improving voluntary muscle control and methods of treating neuropathic pain in a subject having an injury to the nervous system. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

Abstract: Pure crystalline forms of 1-benzyl-N-(4-carbamimidoylbenzyl)-1H-pyrazole-4-carboxamide acetate, and an amorphous form, pharmaceutical compositions thereof, and methods for making the same, are disclosed.

Abstract: The present disclosure provides compounds, pharmaceutical compositions, and methods for the treatment of cancer and fibrosis. The disclosed pharmaceutical compositions may include one or more pyrazolyl-containing compounds, or a derivative thereof.

Abstract: The present invention relates to methods for treating patients with compensated cirrhosis, comprising administering to a patient in need thereof a therapeutically effective amount of a soluble guanylate cyclase (sGC) activator, or a pharmaceutically acceptable salt thereof.

Abstract: The present disclosure generally relates to compounds class I HDAC inhibitors, their production and applications. The compounds possess epigenetic immunomodulatory activities in the tumor microenvironment (TME) and thus inhibit growth of tumor cells.

Abstract: Disclosed are compounds of Formula I: or a pharmaceutically acceptable salt, a solvate, a tautomer, a stereoisomer or a deuterated analog thereof, wherein R1, R2, R3, A, E, L, and G are as described in any of the embodiments described in this disclosure; compositions thereof; and uses thereof.

Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, as defined in the specification. In an embodiment, a pharmaceutical composition can be in a liquid dosage form and can comprise a therapeutically effective amount of the compound or a pharmaceutically acceptable salt thereof as an adjuvant and a therapeutic agent. In another embodiment, a method of adjuvant treating a disorder or condition can comprising administering the pharmaceutical composition to a patient.

Abstract: Provided herein are methods of treating heart failure in patients exhibiting one or more additional features, comprising administering to the patient a therapeutically effective amount of omecamtiv mecarbil, or a hydrate, salt, or salt of a hydrate thereof.

Abstract: This application describes methods of treating cystic fibrosis or a CFTR mediated disease comprising administering Compound I or a pharmaceutically acceptable salt thereof. The application also describes pharmaceutical compositions comprising Compound I or a pharmaceutically acceptable salt thereof and optionally comprising one or more additional CFTR modulating agents.

Abstract: The invention provides synthetic intermediates and synthetic processes that are useful for preparing the antibacterial agent TXA709: