Azetidines are an important class of saturated four-membered nitrogen-containing heterocyclic compounds. The research hotspots related to this structure mainly focus on two aspects: one is the research of pharmaceutical chemistry; the other is related to chiral azetidines, using rigid azetidine compounds as chiral ligands for asymmetric catalytic reactions. Many nitrogen-containing heterocycles play important roles in drug structures, and in many cases small structural changes can improve ligand selectivity and pharmacokinetic properties.
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When the ends of the chains are joined together into a ring, cyclic compounds result; such substances often are referred to as carbocyclic or alicyclic compounds. Substitution of one or more of the ring carbon atoms in the molecules of a carbocyclic compound with a heteroatom gives a heterocyclic compound.
Giredestrant (GDC-9545) is under development by Roche/Genentech. Giredestrant is a potent, next generation investigational selective oestrogen receptor (SERD) with best-in-class potential. In the phase 2 coopERA trial, postmenopausal patients with untreated ER+/HER2- early breast cancer were randomly assigned to receive neoadjuvant combination therapy with palbociclib and giredestrant or anastrozole, followed by surgical intervention within 14 days. The tumor biomarker Ki67 of the patients was ≥ 5% when they were enrolled in the group. The analysis showed that patients receiving giredestrant combination therapy (mean Ki67 reduction of 80%) had a greater mean reduction in Ki67 levels from baseline at week 2 compared with anastrozole combination therapy (mean Ki67 reduction of 67%). The pivotal phase 3 trial of giredestrant is recruiting patients and preliminary data is expected in 2025. Chemenu has been working to develop more compounds for drug discovery. Here are the building blocks we can provide.
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