MEDICINE COMPRISING ACETIC ACID AMIDE DERIVATIVE

• Main Authors: HINO KATSUHIKO, ITOU MARI, OKA MAKOTO, MURATA AKICHIKA, FURUKAWA KIYOSHI
• Format: Patent
• Language: English
• Published: 19.05.1998
• Edition: 6
• 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

PROBLEM TO BE SOLVED: To obtain a medicine selectively and strongly acting on a peripheral benzodiazepine receptor, comprising a specific acetic acid amide derivative (acid addition salt) as an active ingredient. SOLUTION: This medicine comprises an acetic acid amide derivative (acid addition salt) of formula I [X is O or NR4 (R4 is H, a lower alkyl, etc.); R1 is H, a lower alkenyl, etc.; R2 is a lower alkyl, a cycloalkyl, etc., or R1 and R2 together with adjoining N form a group of formula II (A is a single bond, NH, etc.; Ra and Rb are each H, a lower alkyl, etc.); R3 is H, a hydroxy (lower) alkyl, etc.; R5 is H, a lower alkenyl, etc.; R6 is H, trifluoromethyl, etc.; R7 is H, OH, etc.; R8 is H, halogen, etc.]. The compound of formula I is obtained by reacting a compound of formula III (Z is an eliminable atom or an eliminable group; R51 is R5 containing a protected amino, etc.) with a compound of formula IV (R31 is H, a lower alkyl, etc.) and optionally eliminating the protection group of the reaction product.