Piperazine is an organic compound consisting of a six-membered ring containing two nitrogen atoms in opposite positions in the ring. The chemical formula of piperazine is C4H10N2, and it is an important pharmaceutical intermediate. Pyrimidines and piperazines are known to be the backbone of many bulk compounds and important core structures for approved drugs; studies have shown that combining a pyridine ring with a piperazine moiety within a single structural framework enhances biological activity.
Oxygen heterocycles are one of the most common heterocycles in drugs and natural products. Oxetene has high polarity and is also a good acceptor for hydrogen bond, which contributes to the metabolism and chemical stability of its host molecules. When substituted for commonly used functional groups such as gem dimethyl or carbonyl, oxetane units can induce profound changes in water solubility, lipophilicity, metabolic stability and conformational preference. Four of the FDA-approved drugs contain oxetenes: Orlistat, Paclitaxel, and two of its derivatives, Docetaxel and Cabazitaxel. Currently, oxetane-containing building blocks are flourishing in medicinal chemistry and drug discovery.
Positive results from the Phase 2 study RILECSU showed that rilzabrutinib significantly improved itch, hives and urticaria in adults with moderate-to-severe chronic spontaneous urticaria (CSU), whose symptoms are not adequately controlled by H1 antihistamines. These results were released at the 2024 American Academy of Allergy, Asthma, and Immunology (AAAAI) Annual Meeting and form the basis for the Phase 3 program which is on track to start in 2024. Rilzabrutinib is an oral, reversible, covalent BTK inhibitor that has the potential to be a first- or best-in-class treatment of a number of immune-mediated diseases. Chemenu has been working to develop more compounds for drug discovery. Here are the building blocks we can provide.
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