Over the past 20 years, leading pharmaceutical companies (BMS, Takeda, Merck & Dohme, etc) have shown increasing interest in saturated conformationally rigid bicyclic fused sultams, which exhibit remarkable anticancer activity and have been studied as potential antischizophrenic and antithrombotic agents (Figure ). The vast majority of synthesized and patented sultams are decorated with a fused saturated sulfonamide fragment. Notable examples of of [m.n.0]sultams include an antischizophrenic agent 13, an antithrombotic agent 14, an anticancer agent 15, a proteaseactivated receptor 1 (PAR-1 ) antagonist 16, a γ-secretase inhibitor 17, and a casein kinase II inhibitor 18. Conversely, bicyclic bridged and spirocyclic sultams are less studied, likely due to the limited number of synthesized representatives to date, and the scarcity of described preparation methods compared to their fused counterparts. This chemotype is represented by a human immunodeficiency virus protease inhibitor 19 and a related orphan retinoic acid receptor-related orphan receptor  46 (RORγ) inhibitor 20.