Orvepitant is a novel generation brain penetrant, selective and potent, small molecule NK-1 receptor antagonist. Orvepitant’s (GW823296) mode of action and developability characteristics made it a suitable development candidate for the treatment of common anxiety disorders, posttraumatic stress disorder and major depressive disorder. It’s in phase II clinical trials as an effective inhibitor of itch-associated response.

ISOMAZOLE is a cardiovascular agent with both inotropic and vasodilator activities. It acts primarily as a phosphodiesterase inhibitor.

Pamatolol is a beta-Adrenergic receptor antagonist was studied as an Antiarrhythmic agent. The phase I clinical trial has shown that the drug was relatively cardioselective in man. Information about the further development of this drug is not available.

Pargeverine (also known as a propinox) is an antispasmodic drug that was studied for the treatment of disorders of the gastrointestinal tract, the uterus, and the gallbladder. Pargeverine showed a dual mechanism of action, it binds to muscarinic and calcium receptors that can be related to its antispasmodic activity. The clinical trial has shown that pargeverine was an effective drug in the treatment of moderate to severe colic pain of biliary origin. In addition, its efficacy and tolerability were determined in patients with moderate-to-severe acute intestinal colic pain. As a result, no differences in blood pressure or heart rate were found among treatments. The incidence of mouth dryness was significantly more frequent with the 20 mg and 30 mg doses of propinox than with the placebo or the 10 mg dose. Information about the current development of this drug is not available.

Enpiroline (WR 180,409) is an antimalarial compound. It demonstrates activity against Plasmodium falciparum both in vitro and in non-immune infected subjects. Additionally, it exerts antischistosomal activity.

Denaverine is a benzilacid derivative. It is a phenobarbital-type microsomal enzyme inducer. Denaverine has a relaxing effect on the prepartum uterus and provides an increased flexibility of the soft birth canal. In addition, it has a surface anaestetic effect and an anticonvulsive effect as well as a slightly tranquilizing and antipyretic effect. In veterinary medicine denaverine hydrochloride is used to regulate myometrial contractions during parturition. It is a regularly used substance in obstetrics in veterinary medicine in many European countries.

Clocinizine is an antihistamine derivative of diphenylmethylpiperazine. Clocinizine is a competitive and reversible H1 receptor antagonist. The drug is marketed in Spain under tradename Senioral in combination with phenylpropanolamine for temporary relief of nasal congestion in colds, rhinitis, and sinusitis.

Quinuclium Bromide Anhydrous is quinuclidinium derivative with potential analgesic activity. In preclinical studies, Quinuclium possessed significant chronic antihypertensive activity in mecamylamine- and renal-hypertensive dogs. Quinuclium was approximately 4 times more potent than guanethidine in the former model and 3 times as potent in the latter. Quinuclium reduced orthostatic blood pressure responses in unanesthetized rabbits but was approximately 10 times less potent than guanethidine. Quinuclium did not affect cardiac output, heart rate or stroke volume in anesthetized open-chest dogs and moderately increased mean blood pressure and total peripheral resistance. It produced diuresis and saluresis in anesthetized dogs but did not influence water or electrolyte urinary excretion in conscious rats. Quinuclium was more effective than guanethidine in blocking adrenergic neurons and depleting heart norepinephrine levels in experimental animals.

Mocetinostat is an rationally designed, orally available, Class 1-selective, small molecule, 2-aminobenzamide HDAC inhibitor with potential antineoplastic activity. Mocetinostat binds to and inhibits Class 1 isoforms of HDAC, specifically HDAC 1, 2 and 3, which may result in epigenetic changes in tumor cells and so tumor cell death; although the exact mechanism has yet to be defined, tumor cell death may occur through the induction of apoptosis, differentiation, cell cycle arrest, inhibition of DNA repair, upregulation of tumor suppressors, down regulation of growth factors, oxidative stress, and autophagy, among others. It is undergoing clinical trials for treatment of various cancers including bladder cancer, diffuse large B cell lymphoma, follicular lymphoma, myelodysplastic syndromes, non-small cell lung cancer. Fatigue, weight loss or anorexia were most common treatment-related adverse events.