54 results about "Glutaminyl cyclase" patented technology

A novel crystal structures of human and murine glutaminyl cyclase (QC, EC 2.3.2.5), methods of preparing the crystals, as well as the use of said crystal structures for identifying inhibitors of human and murine glutaminyl cyclase.

The invention relates to chemistry of organic substances, pharmacology and medicine, and concerns treating diseases associated and with aberrant activity of cells of the immune system, more particularly for treating lung, respiratory tract and abdominal diseases, radiation sickness, pain syndrome and other diseases by using compounds of formula (A), wherein R1 is a -C(O)-R2-C(O)- or -R2-C(O)- group, where R2 is a -(CH2)n- group optionally substituted with one or two C1-C6 alkyls, or phenyl, and n is an integer from 0 to 4; wherein the compounds are selected from a group consisting of the compounds as set out in the description. These compounds, as well as pharmaceutically acceptable salts thereof, are highly effective in inhibiting glutaminyl cyclase, which is involved, in particular, in post-translational modification of chemokines and chemotaxis of monocytes, macrophages and other cells of the immune system. This invention also relates to pharmaceutical compositions comprising a therapeutically effective amount of the compounds of formula (A) as defined above.

The invention discloses a synthesis method and application of a multi-target A beta oligomerization inhibitor. The synthesis method comprises the following steps: (1) taking bromaniline or derivatives thereof and (1-benzylpiperidine-4-yl)methylamine or derivatives thereof as starting raw materials, and carrying out Suzuki coupling reaction for preparing an intermediate II; (2) taking the intermediate II and 1,3-dibromopropane or other analogues as raw materials, and carrying out SN2 reaction for preparing an intermediate III with an alkyl chain; and (3) taking the intermediate III with the alkyl chain and imidazole or derivatives thereof as raw materials, and carrying out SN2 reaction for preparing the target product multi-target A beta oligomerization inhibitor. The synthesis method disclosed by the invention is simple and reliable in route, high in yield and more suitable for large-scale preparation. The multi-target A beta oligomerization inhibitor is applied to preparation of an A beta oligomerization inhibitor anti-AD medicine, a glutaminyl cyclase inhibitor anti-AD medicine and an acetylcholin esterase inhibitor anti-AD medicine and can be applied to kits of A beta oligomerization, glutaminyl cyclase and acetylcholin esterase.