Piperidine is an azacycloalkane that is cyclohexane in which one of the carbons is replaced by a nitrogen. Although piperidine is a common organic compound, it is an immensely important class of compounds medicinally: the piperidine ring is the most common heterocyclic subunit among FDA approved drugs.
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Morpholine contains secondary amine groups and has all the typical reactive characteristics of secondary amine groups. It can react with inorganic acids to form salts, and react with organic acids to form salts or amides, which can be subjected to alkylation reaction, and can also be reacted with ethylene oxide, ketone or Willgerodt reaction. Morpholine is a six-membered ring containing oxygen and nitrogen, and its alkalinity is much lower than that of its parent piperidine. The marketed morpholine drugs are mainly distributed in the fields of tumors, cardiovascular and cerebrovascular diseases, respiratory system diseases, digestive system diseases, infectious diseases and mental disorders.
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Genentech, a member of the Roche Group, has announced that its ALK inhibitor Alecensa® (Alectinib) met its primary endpoint of disease-free survival (DFS) at a scheduled interim analysis of the phase 3 ALINA trial. Alecensa as adjuvant therapy resulted in statistically significant DFS and clinically meaningful improvement.
Worldwide, lung cancer is one of the most common cancers, with NSCLC accounting for 80% to 85% of all lung cancer cases. Despite adjuvant chemotherapy, about half of patients with early-stage lung cancer experience cancer recurrence after surgery. Recent therapeutic innovations, including immunotherapy, have improved the outlook for some patients with early-stage NSCLC; however, there are currently no ALK inhibitors approved for early-stage ALK-positive disease. Alecensa is the first ALK inhibitor proven in a Phase 3 trial to reduce the risk of disease recurrence or death in patients with early-stage ALK-positive NSCLC. Chemenu has been working to develop more compounds for drug discovery. Here are the building blocks we can provide.