Clantifen is an aminothiophene derivative invented by Hoersht AG. The compound is claimed to have antiphlogistic and antipyretic properties.

Sinefungin, a natural nucleoside isolated from cultures of Streptomyces incarnatus and S. griseolus, is structurally related to S-adenosylhomocysteine and S-adenosylmethionine. Sinefungin is a DNA methyltransferase (DNMT) inhibitor (IC₅₀ = 0.1 - 20 uM). Sinefungin has been shown to inhibit the development of various fungi and viruses, but its major attraction to date resides in its potent antiparasitic activity. This compound has been reported to display antiparasitic activity against malarial, trypanosomal, and leishmanial species. Sinefungin inhibits pneumococcal biofilm growth in vitro and colonization in vivo, decreases AI-2 production, and downregulates luxS, pfs, and speE gene expressions. Sinefungin was significantly suppressive against both L. donovani and L. braziliensis panamensis infections in hamsters when compared with meglumine antimonate. An immunosuppressed rat model was used to investigate the anti-Cryptosporidium parvum activity of sinefungin. In infected animals, oral sinefungin therapy resulted in a dose-related suppression of oocyst shedding, which correlated with oocyst disappearance from ileal sections. When administered prior to or on the day of oocyst challenge, sinefungin successfully prevented infection. These data suggest that sinefungin could be considered as a candidate molecule in the treatment of human cryptosporidiosis, considered to be the most significant enteric opportunistic infection in AIDS.

2-Cyano-3,12-dioxooleana-1,9-diene-28-oic acid (CDDO, also known as Bardoxolone) is a synthetic triterpenoid that displays potent anti-inflammatory and antitumorigenic activities. CDDO was in the clinical trial phase I for the treatment patients with Solid tumors and leukemia, but that studies were discontinued. It is known, that CDDO blocks the cellular synthesis of inducible nitric oxide synthase and inducible COX-2. In addition, was discovered, that CDDO disrupted intracellular redox balance and thereby induce apoptosis. Moreover, CDDO is a ligand for peroxisome proliferator-activated receptor that it induces genes regulated by Nrf2, including heme oxygenase-1 and eotaxin-1, which play a role in antioxidant response element signaling activity.

M40419 (now GC4419) is a Mn(II)-containing pentaazamacrocyclic selective superoxide dismutase mimetic. It is a first-in-class, small molecule enzyme mimetic that converts superoxide to hydrogen peroxide and molecular oxygen. GC4419 is currently being evaluated in an ongoing randomized Phase 2 clinical trial to assess its effect on the incidence, severity and duration of severe oral mucositis (OM) when given to patients with squamous cell cancers of the head and neck in combination with radiation and chemotherapy. GC4419 has received Breakthrough Therapy and Fast Track designations from the U.S. Food and Drug Administration.

Ciluprevir (BILN-2061) is a selective inhibitor of the HCV NS3 serine protease, which was developed by Boehringer Ingelheim for the treatment of hepatitis C infection. The drug was discontinued in phase II due to adverse events such as cardiac toxicity (demonstrated in animals). In the cell-based replicon assay, ciluprevir inhibited HCV RNA replication at low nanomolar levels. It had inhibitory rate constant (Ki) values of 0.3 and 0.66 nM for the NS3 proteases of HCV genotypes 1a and -1b, respectively.

Metethoheptazine (WY-535) is an analgesic agent.

BMS-908662 (previously known as XL281) is a small molecule Raf kinase inhibitor that lies immediately downstream of RAS and are key components of the RAS/RAF/MEK/ERK kinase-signaling pathway. Bristol-Myers Squibb has received an exclusive worldwide license to develop and commercialize antineoplastic agent XL281. BMS-908662 participated in phase I development for the treatment of patients with melanoma and in combination with cetuximab for patients with colorectal cancer. However, further, development has been discontinued.

LANPROSTON is an analog of prostaglandin F2 alpha. It is used as veterinary medicament.