Provided are processes for the preparation of (S)-tert-butyl 4,5-diamino-5-oxopentanoate, or a salt, solvate, hydrate, enantiomer, mixture of enantiomers, or isotopologue thereof. Also provided are solid forms of various intermediates and products obtained from the processes.

The present invention relates to use of peptides as a therapeutic agent, wherein it has been confirmed that the peptides of the present invention significantly inhibit the activity of T cells and the differentiation of T helper 17 cells (Th17 cells), which are associated with autoimmune disease, and have remarkable effects of treating and improving arthritis in an animal model of arthritis. Therefore, the peptides may be used as an active ingredient in therapeutic agents for various autoimmune diseases such as bone disease, inflammatory disease or rheumatoid arthritis.

The invention relates to a process for preparing immediate precursors for pyroxasulfone and fenoxasulfone preparation of the formula (I). The process comprises a bromination of a benzylic position without light irradiation, followed by thoination, which substitutes the bromine atom and after the protecting group is removed, and the revealed thiol or thiolate reacts with a substituted isoxazoline bearing a leaving group at the 3-position. Alternately, the pyroxasulfone or fenoxasulfone immediate precursor is synthesized from arylmethyl bromide by forming a carbon-sulfur bond at the 3-position of a 2-isoxazoline through displacement of a leaving group at the 3-position by an appropriate thionating reagent. The resulting adducts, which is a S-protected 3-thio-2-isoxazoline, may be treated with base to remove the protecting group, to reveal a thiol or thiolate which may subsequently react with the arylmethyl bromide to form the Pyroxasulfone or Fenoxasulfone immediate precursor.

The present invention relates to a novel gadolinium-based compound having a structure in which a gadolinium complex and a gallic acid are bonded to each other, a method for producing same, and an MRI contrast agent containing same.

The present invention relates to a novel morpholino oligonucleotide comprising at least one type of morpholino nucleotide monomer having pyrrolocytosine (pC) among unnatural cytosines, and relates to a morpholino oligonucleotide capable of more selectively binding to a target RNA and exhibiting excellent cell penetration compared to an MPO having a natural cytosine, and thus being capable of greatly contributing to the development of a therapeutic agent for incurable diseases in the area of morpholino oligonucleotides.

A nitrogen-containing ring derivative regulator, a preparation method therefor and use thereof. In particular, the present invention relates to a compound as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and use thereof as a G protein-coupled receptor regulator in the treatment or prevention of central nervous system diseases and/or mental diseases.

##STR00001##

This fluorine-containing ether compound is represented by formula (1) shown below.

R.sup.1—CH.sub.2—R.sup.2—CH.sub.2—R.sup.3  (1)

In formula (1), R.sup.2 is a perfluoropolyether chain represented by a formula (2) shown below. R.sup.1 is a terminal group that is bonded to R.sup.2 via a CH.sub.2 group, and is represented by a formula (3) shown below. R.sup.3 is bonded to R.sup.2 via a CH.sub.2 group, is a terminal group having at least one hydroxyl group, and may be the same as, or different from, R.sup.1.

—(CF.sub.2).sub.p-1—O—((CF.sub.2).sub.pO).sub.q—(CF.sub.2).sub.p-1—  (2)

In formula (2), p represents an integer of 2 to 3, and q indicates the average polymerization degree and is a number within a range from 1 to 20.

—O(CH.sub.2—CH(OH)—CH.sub.2—O).sub.2—CH.sub.2—(CH.sub.2).sub.n,—OH  (3)

In formula (3), n represents an integer of 1 to 8.

The present invention relates to a spiro ring-containing quinazoline compound, a preparation method therefor, and use of the compound as a K-Ras G12C inhibitor in preparing antitumor medicaments.

##STR00001##

The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TRβ mutation.

Provided are lincosamide compounds for the treatment of infectious diseases. The lincosamides described herein are modified at the C-7 position of the aminooctose (northern) region, thus distinguishing them from lincomycin and clindamycin. Also provided are methods for preparing the lincosamide compounds, pharmaceutical compositions comprising the lincosamide compounds, and methods of treating infectious diseases using the disclosed lincosamide compounds.