Cyclopropane is the smallest cyclic compound with unique structural features and physicochemical properties, which is widely used in the design of small molecule drugs. In drug design, it is often used to increase activity, fix conformation and improve PK and water solubility. The introduction of cyclopropyl groups into drugs can change various properties of molecules, such as improving metabolic stability; increasing biological activity; enhancing drug efficacy; limiting polypeptide conformation and slowing down its hydrolysis; reducing plasma clearance; improving drug dissociation and many more. Cyclopropane rings are widely found in marketed drugs, including cardiovascular drugs, central nervous system (CNS) drugs, anticancer drugs, autoimmune and anti-inflammatory drugs.
Novartis announced new positive data from the Phase III REMIX-1 and REMIX-2 studies investigating remibrutinib - a highly selective, oral Bruton's tyrosine kinase (BTK) inhibitor - in people with chronic spontaneous urticaria (CSU) whose symptoms are inadequately controlled by H1-antihistamines. In the studies, remibrutinib met all primary and secondary endpoints at Week 12. Remibrutinib is a potential 'best-in-class' BTK inhibitor. It can covalently bind to the BTK enzyme of B cells and myeloid cells. While strongly inhibiting BTK activity, it reduces the systemic exposure of the drug and reduces the risk of adverse events and drug interactions. Chemenu has been working to develop more compounds for drug discovery. Here are the building blocks we can provide.
検索 
+86 21 5895 0110 
