LACTAM DERIVATIVE

PROBLEM TO BE SOLVED: To obtain a new lactam derivative which has the interleukin-1β production-inhibitory action and the tumor necrosis factor α-liberation-inhibitory action and is useful as a therapeutic agent for rheumatoid arthritis and septicemia. SOLUTION: This lactam derivative is represented...

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Hauptverfasser:	ARIGA MASATO, KATSUYAMA KOICHI, MAGAI AKIKO, YANAI MAKOTO, SAITO YUKIO, HATANAKA SHIGEO, YOKOYAMA SHINJI, SUEDA NORIYOSHI, MURANAMI CHIKAKO, MOMOSE KENICHI, YAMADA HIROAKI
Format:	Patent
Sprache:	eng
Schlagworte:	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
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Beschreibung
Zusammenfassung:	PROBLEM TO BE SOLVED: To obtain a new lactam derivative which has the interleukin-1β production-inhibitory action and the tumor necrosis factor α-liberation-inhibitory action and is useful as a therapeutic agent for rheumatoid arthritis and septicemia. SOLUTION: This lactam derivative is represented by formula I (Het is pyridyl; X is C, O; n is 1-4; R is H, a 1-4C alkyl where the cases of n=1, X=C, and R=H are excluded), typically 1-[3-(3-pyridyl)-acryloyl]-2-piperidinone. The compound of formula I is obtained by reaction of a carboxylic halide of formula II (Hal is a halogen) with a lactam of formula III in the presence of a base.