5 results about "Aza Compounds" patented technology

The invention discloses a benzo-aza compound as well as a preparation method and application thereof. The benzazepine compound and the pharmaceutically acceptable salt of the benzazepine compound prepared by the invention have relatively high sensitivity and very strong cytotoxic activity to human colon cancer cells HCT116 tumor cells. The triethylene diamine catalyst is adopted in the process of preparing the benzo-aza compound, the reaction conditions are relatively conventional, the reaction process is mild, simple and convenient, the operation is easy, the cost is low, and the method is suitable for industrial large-scale production; according to the method, various substrates are used as reactants, products with various and complex structures are obtained, the yield is high, and the application range of the method is widened. The compound prepared by the preparation method disclosed by the invention has relatively high cytotoxic activity on human colon cancer cells HCT116. Therefore, the preparation method provided by the invention can provide a basis for screening the benzazepine compound with good activity on tumor cells, and is beneficial to further screening out compounds with more excellent biological activity.

The invention relates to 1,5-benzothiazepine and 1,2,5-benzothiadiazepine derivatives of formula (I). These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and / or liver bile acid transport (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases.

The present application relates to the field of organic synthesis, and is a preparation method of imidazo six-membered nitrogen heterocyclic compounds containing isothiourea fragments for medicines and intermediates. The method uses nitrogen atom ortho isocyanomethyl-substituted pyridine, pyrimidine, pyrazine, quinoline and other nitrogen-containing heteroaromatic rings as raw materials, reacts with various disulfides under the action of N-chlorosuccinimide (NCS) and a catalytic amount of TEMPO, and intramolecularly cyclizes to form imidazo six-membered nitrogen heterocyclic compounds containing isothiourea fragments. The method can realize intramolecular ring closure in one step, form imidazo[1,5a] nitrogen-containing heteroaromatic rings containing isothiourea fragments, construct various imidazo[1,5a] nitrogen-containing heteroaromatic rings containing isothiourea fragments, has high yield, low raw material cost, can realize large-scale industrial production, and has market application prospect.

Compound of formula (l): wherein R1 represents a hydrogen atom or a heterocyclic, cyano, alkoxycarbonyl, alkylsulphoriylaminoalkyl or N-hydroxycarboximidamide group, process for its preparation and pharmaceutical composition containing it for use as a modulator of the AMPA (a-amino-3 hydroxy-5 -methyl-4-isoxazole-propionfc acid) receptor.

The present disclosure provides, in part, benzothia(dia)zepine compounds, and pharmaceutical compositions thereof, and methods of treating Hepatitis B virus (HBV) and Hepatitis D virus (HDV) infections.