A spiro compound is a polycyclic compound in which two monocyclic rings share one carbon atom; the shared carbon atom is called a spiro atom. Spiro compounds have rigid structures, stable structures, and have special properties that general organic compounds do not possess, such as anomeric effect, spiro conjugation and spiro hyperconjugation. Compared with the monocyclic structure or the planar aromatic structure, the spiro structure has a larger three-dimensional structure; the heterocyclic spiro structure is also regarded as the biological isostere of some groups, which can change the drug to a certain extent. The water solubility, lipophilicity, dominant conformation and ADMET properties of the molecule make the optimized lead molecule easier to drug. Therefore, spiro compounds occupy a very important position in drug development.
Spiro And Bicyclic Compound
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Pyrrolidine, also known as tetrahydropyrrole, is a saturated five-membered heterocyclic ring, which is miscible with water. Pyrrolidine exists in many alkaloids and drug molecules, such as kappa opioids, antagonists of dopamine D4 receptors, and HIV reverse transcriptase inhibitors.
Revolution Medicines announced preliminary positive data for its RAS(ON) G12D-selective covalent inhibitor RMC-9805 in previously treated pancreatic ductal adenocarcinoma (PDAC) patients. The analysis showed that the disease control rate of PDAC patients treated with RMC-9805 was as high as 80%. RMC-9805 is a potential ‘first-in-class’ oral RAS(ON) G12D-selective inhibitor, that is being evaluated in trials to examine its efficacy and safety in patients with solid tumors carrying KRAS G12D mutations when used as a single agent or in combination with the pan-RAS inhibitor RMC-6236. Chemenu has been working to develop more compounds for drug discovery. Here are the building blocks we can provide.
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