159603-71-1Relevant articles and documents
PYRIMIDINE-FUSED CYCLIC COMPOUND, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
-
Paragraph 0515-0517; 0972-0974, (2021/02/26)
Disclosed in the present disclosure are a pyrimidine-fused cyclic compound or a pharmaceutically acceptable salt, hydrate, prodrug, stereoisomer, solvate or isotope labeled compound thereof. Also provided in the present disclosure are a preparation method for the compound, a composition comprising the compound and a use of the compound for the preparation of a medicament for the prevention and/or treatment of a disease or condition associated with abnormal SHP2 activity.
Pyridoazepine derivative, pharmaceutical composition and applications thereof
-
Paragraph 0125-0127, (2019/05/16)
The present invention discloses a pyridoazepine derivative, a pharmaceutical composition and applications thereof, wherein the pyridoazepine derivative (I), the isomer, the prodrug, the stable isotopederivative or the pharmaceutically acceptable salt thereof have the following structure. According to the present invention, the pyridoazepine derivative has good regulatory effects on TLR family andrelated signaling pathways, particularly on TLR8, can effectively treat, alleviate and/or prevent various diseases mediated by signaling pathways related to TLR family and TLR, and particularly can effectively treat, alleviate and/or prevent various TLR8 mediated diseases such as cancers, autoimmune diseases, infections, inflammations, transplant rejections, graft versus host diseases and the like. The formula (I) is defined in the specification.
A Filgotinib synthetic method
-
Paragraph 0029; 0030; 0042; 0049; 0056, (2017/08/25)
The invention discloses a filgotinib synthetic method and belongs to the technical field of chemical synthesis of medicines. 6-chloro-2-aminopyridine and di-tert-butyl dicarbonate ester are subjected to condensation reaction to obtain 6-chloro-2-tert-butyloxycarbonyl aminopyridine; hydrolysis reaction is performed; the obtained 6-chloro-2-tert-butyloxycarbonyl aminopyridine and trifluorinated methyl sulfonic anhydride are subjected to trifluoromethanesulfonic acid esterification reaction; the obtained 2-tert-butyloxycarbonylamino-6-pyridyltrifluoromethanesulfonate and [(1,1-dioxo-4-thiomorpholinyl)methyl]benzo-4-boronic acid pinacol ester are subjected to condensation reaction to obtain a tert-butyl ester derivative; the tert-butyl ester derivative is treated by trifluoroacetic acid and subjected to de-protection; the obtained intermediate and ethoxycarbonyl isothiocyanate are subjected to isothiocyanate reaction; the obtained intermediate and hydroxylamine hydrochloride are subjected to ring closing reaction; the obtained intermediate and cyclopropane carbonyl chloride are subjected to amidation reaction to obtain the finished product. Operation is simplified; reagents are available; the concept of environment friendliness and environment protection is embodied.