URB-597 (KDS-4103) is a highly potent and selective inhibitor of the enzyme fatty acid amide hydrolase (FAAH), which catalyzes the intracellular hydrolysis of the endocannabinoid anandamide. URB597 is one the best studied carbamate-based inhibitors. Early studies showed that the compound did not inhibit or bind related biological targets. Administration of URB597 to rats and subsequent in vivo evaluation of brain FAAH activity showed the compound elevated endogenous anandamide levels. Importantly, the compound did not produce catalepsy, hypothermia, or hyperphagia, three of the typical effects of exogenous cannabinoids. The compound did produce antinociceptive effects in the mouse hot-plate test, which were reversed by the CB1 antagonist rimonabant. These findings again support the expectation that inhibition of FAAH produces pharmacology distinct from an exogenous CB1 agonist. A more detailed study was published later showing time-course data in mice demonstrating elevation of anandamide, oleamide, and N-palmitoyl ethanolamine for 2–6 h after administration of URB597. In vivo administration of URB597 showed almost complete inhibition of FAAH by the compound, and the FAAH inhibition was still approximately 70% after 16 h. Complete recovery of CNS FAAH activity was observed 24 h after administration of URB597. In vivo administration of URB597 or the cannabinoid receptor agonist HU210 reduced both mechanical allodynia and thermal hyperalgesia in the CFA model of inflammatory pain. Effects in the inflammatory model were partially reversed by CB1 and CB2 antagonists. In a related study, the compound produced analgesic effects in the mouse CCI model (neuropathic) when administered orally. These effects were also reversed by both CB1 and CB2 antagonists.

Bristol-Myers Squibb developed BMS-929075 as a selective, orally bioavailable hepatitis C virus (HCV) NS5B polymerase inhibitor for the treatment of chronic HCV infection. BMS-929075 was involved in phase I clinical trials for hepatitis C virus (HCV) infected patients; however, the company withdrew a study prior to enrolment.

Nacubactam (FPI-1459) was developed as an antibacterial drug. Nacubactam successfully has completed phase I clinical trials for the treatment of serious gram-negative bacterial infections. The drug is currently being developed for the treatment of complicated urinary tract infection, hospital-acquired bacterial pneumonia, ventilator-associated bacterial pneumonia, and complicated intra-abdominal infections. FPI-1459 works through several mechanisms of action, inhibiting a number of beta-lactamase enzymes as well as certain bacterial cell wall enzymes. In January 2019, FPI-1459 received Fast Track and Qualified Infectious Disease Product designations from the U.S. Food and Drug Administration (FDA).

(S,R)-3-Phenyl-4,5-dihydro-5-isoxasole acetic acid (VGX-1027, GIT-027) is an isoxazole compound that exhibits various immunomodulatory properties. This compound reduced the secretion of IL-1beta, TNF-alpha and IL-10 from purified murine macrophages stimulated "in vitro" with lipopolysaccharide (LPS), and it also modified the signaling pathways induced in these cells by LPS entailing reduced activation of NF-kappaB and p38 MAP kinase pathways along with up-regulation of ERK pathways. The animals receiving VGX-1027 exhibited reduced production of the proinflammatory mediators tumor necrosis factor-alpha, IL-1beta, macrophage migration inhibitory factor, and inducible nitric-oxide synthase-mediated nitric oxide generation in both pancreatic islets and peripheral compartments. Inovio Pharmaceuticals is developing VGX-1027 for the treatment of inflammatory conditions such as rheumatoid arthritis, type 1 diabetes mellitus, uveitis and ulcerative colitis.