2 results about "Laquinimod" patented technology

The invention discloses a nitrogen-containing heterocyclic carboxylic acid compound as well as a preparation method and application thereof, and belongs to the technical field of organic synthesis. According to the present invention, CO2 is adopted as the carboxyl source, the raw materials such as the 4-hydroxypyridine or 2-pyridone compound and the alkali are subjected to the simple heating reaction to prepare the nitrogen-containing heterocyclic carboxylic acid compound, and the method has characteristics of mild reaction condition, wide reaction substrate range, good yield, good chemical selectivity and the like; according to the present invention, the efficient and convenient synthesis of various heterocyclic carboxylic acid compounds is achieved, the obtained product can further prepare various drugs and intermediates such as oxolinic acid, etofaka, laquinimod and the like, and the synthesis route has advantages of simple and easily available raw materials, mild reaction conditions, high yield, simple and convenient post-treatment, good atom economy, and suitableness for large-scale preparation.

This invention discloses the application of elamod in the preparation of drugs for treating neuromyelitis optica spectrum disorders (NMOSD). For the first time, in vivo animal experiments have demonstrated that elamod can significantly inhibit the production of pathogenic AQP4 antibodies in NMOSD model mice, improve motor function, retinal and optic nerve function, and reduce myelin damage. Unlike existing B-cell depletion monoclonal antibody therapies, elamod employs a "non-depletion" regulatory mode, inhibiting B-cell activation and antibody secretion without directly eliminating B cells, thus preserving some immune surveillance function and reducing the risk of long-term infection. Ailamod is an oral small molecule drug, included in the national medical insurance program, inexpensive, with no immunogenicity risk, and significantly better patient compliance than injectable monoclonal antibodies. This invention provides a novel, highly effective, and specific targeted drug for NMOSD, possessing significant clinical translational value.