OXADIAZOLE RING-CONTAINING COMPOUND, PREPARATION METHOD THEREFOR, AND INTERMEDIATE, COMPOSITE, AND APPLICATION THEREOF

• Main Authors: WANG, Qian, XIA, Guangxin, SHU, Sijie, ZHANG, Bingbin, SHI, Chen, ZHANG, Leduo, MAO, Yu, ZHOU, Jialing, CHEN, Na, LIU, Yanjun, ZHANG, Lin
• Format: Patent
• Language: Chinese; English; French
• Published: 26.04.2018
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Disclosed are an oxadiazole ring-containing compound, a preparation method therefor, and an intermediate, a composite, and an application thereof. The oxadiazole ring-containing compound having the formula in the figure below, and a pharmaceutically acceptable salt thereof, an enantiomer thereof, a diastereomer thereof, a tautomer thereof, a solvate thereof, a metabolite thereof, or a prodrug thereof have high IDO inhibitory activity at both molecular and cellular levels, have a significant inhibitory effect on proliferation of tumor cells associated with IDO activity at the animal level, and also have desirable stability against liver microsomes of humans, mice, and other animals, no significant inhibition of metabolic enzymes, good absorption in rats and mice, high bioavailability, and good druggability. L'invention concerne un composé contenant un cycle d'oxadiazole, son procédé de préparation, un intermédiaire, un composite et une application de celui-ci. Le composé contenant un cycle d'oxadiazole ayant l