Coleneuramide (MCC-257) is a cholestane amide conjugate originated in Mitsubishi Pharma Corporation. It has been shown to enhance the effect of nerve growth factor (NGF) on cell survival and on tyrosine phosphorylation in PC12 cells. Coleneuramide is believed to act directly on TrkA receptor. In preclinical models, MCC-257 rescued clinical sign and pathological changes in rats after exposure to environmental neurotoxin methylmercury and protected against dysfunction of the peripheral nervers in hyperglycemic animals. The compound was investigated in phase 2 clinical study for the treatment of diabetic polyneuropathy, but no results were reported.

Cefetecol is a broad-spectrum cephemcarboxylate derivative with antibacterial activity patented by British pharmaceutical company Glaxo Group Ltd.

ABT-510 is an anti-angiogenesis compound that was under development by Abbott for the treatment of solid tumours, lymphoma and melanoma. It is a synthetic peptide that mimics the anti-angiogenic activity of the endogenous protein thrombospondin-1 (TSP-1). ABT-510 inhibits the actions of several pro-angiogenic growth factors important to tumor neovascularization; these pro-angiogenic growth factors include vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF)), hepatocyte growth factor (HGF), and interleukin 8 (IL-8).

Isoindoline pazinaclone (also known as DN-2327), a partial agonist at GABAA benzodiazepine receptors, produced anxiolytic, taming and anti-convulsive effects. This neuropsychiatric drug was involved in phase II clinical trial for patients with generalized anxiety disorder. However, this study was discontinued.

Bidisomide (previously known as SC 40230) was developed as a sodium channel antagonist with class I antiarrhythmic properties. Bidisomide participated in clinical trials for patients with arrhythmia. However, the development was discontinued due to a lack of demonstrable efficacy.

β-N-Acetyl-D-galactosamine (GalNAc) is an amino sugar derived from galactose found in O-linked and N-linked glycans. As an essential sugar, the role is basically the same for N-acetylgalactosamine as it is for the others, which is to enhance cellular communication. Although there has not been much research to date, what has been done reveals that this saccharide may inhibit the growth of some tumors. For example, colon cancer patients have only half the normal amounts of N-acetylgalactosamine. Studies have shown that colon cancer cells that metastasize make more mucin, making them more likely to form metastases. Therefore, it appears that N-acetylgalactosamine plays an important role in preventing this formation from occurring. N-acetylgalactosamine and N-acetylglucosamine glycans is a predictor of metastasis and poor prognosis in a number of human adenocarcinomas, including breast cancer. Lower than normal levels of this sugar has been found in patients with heart disease implying that these conditions may be reversed if a supplementation of N-acetylgalactosamine were to be added to the diet. It appears that β-N-Acetyl-D-galactosamine plays a role in joint function, sweeping away destructive free radicals that can cause inflammation. N-acetylgalactosamine also seems to play an important role in the immune system. Contained in macrophages and neutrophils, it may play a significant role in the etiology of joint inflammation and could be important in such conditions as rheumatoid arthritis. In humans, it is the terminal carbohydrate forming the antigen of blood group A. N-acetylgalactosamine (GalNAc) is a well-defined liver-targeted moiety benefiting from its high affinity with asialoglycoprotein receptor (ASGPR). By conjugating it directly to the oligonucleotides or decorating it to a certain delivery system as a targeting moiety, GalNAc has achieved compelling successes in the development of nucleic acid therapeutics in recent years. Several oligonucleotide modalities are undergoing pivotal clinical studies, followed by a blooming pipeline in the preclinical stage. N-Acetyl-D-galactosamine is used in affinity chromatography, protein chromatography and in carbohydrate matrices. N-Acetyl-D-galactosamine has been used to study periodontal disease and to facilitate the design of potent small-molecule ice recrystallization inhibitors. N-Acetyl-D-galactosamine has also been used to demonstrate a molecular shuttle between extracellular and cytoplasmic space allows for monitoring of GAG biosynthesis.

Paeonol (2-hydroxy-4-methoxyacetophenone) is a major phenolic component of the dried root bark of Paeonia suffruticosa Andrews (Paeoniaceae). Paeonol exhibits a wide variety of bioactivities including anti-inflammatory, antioxidative, immunoregulatory, antihypertensive, anti-hyperglycemic, antibacterial, anti-thrombotic, and antitumor effects. Paeonol inhibits anaphylactic reaction by regulating histamine and TNF-α. Paeonol tablets have been used for the treatment of rheumatic arthritis, fever, headache and neuralgia in Chinese clinics.

Carubicin (also known as Carminomycin) is an anthracycline antineoplastic antibiotic isolated from the bacterium Actinomadura carminata. Carubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. The drug is active against a variety of experimental tumors. Pharmacology studies in animals revealed that the drug bound largely to serum proteins and that it was widely distributed. In clinical trials The main toxic effect was myelosuppression but gastrointestinal intolerance and alopecia were also reported. Objective partial responses were seen in two of seven previously untreated patients with non-small cell lung cancer and one of three patients with squamous cell carcinoma of the head and neck previously untreated with chemotherapy.

Bencisteine was developed as an antitussive, mucolytic agent.