BENZAZEPINE DERIVATIVES USEFUL AS VASOPRESSIN ANTAGONISTS

• Main Authors: YAMADA KEIGO, MENJO YASUHIRO, TOMOYASU TAKAHIRO, TOMOHIRA YUSO, MATSUDA TAKAKUNI, KONDO KAZUMI, MIYAMURA SHIN, KATO YUSUKE
• Format: Patent
• Language: English; Korean
• Published: 21.04.2010
• 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

The present invention provides a benzazepine compound that can maintain for a long period of time the blood level of tolvaptan enabling to provide the desired pharmaceutical effects. The benzazepine compound of the present invention is represented by general formula (1) wherein Rrepresents a-CO-(CH)-CORgroup (wherein n is an integer of 1 to 4, and Ris (2-1) a hydroxy group; (2-2) a lower alkoxy group optionally substituted with a hydroxy group, a lower alkanoyl group, a lower alkanoyloxy group, a lower alkoxycarbonyloxy group, a cycloalkyloxycarbonyloxy group, or 5-methyl-2-oxo-1,3-dioxol-4-yl; or (2-3) an amino group optionally substituted with a hydroxy-lower alkyl group), or the like.