3,4-Dihydro-1H-naphthalene derivatives as a highly selective cyclooxygenase-2 inhibitor

사이클로옥시게나제-2의 저해제로서 선택성이 뛰어난3,4-디하이드로-1h-나프탈렌 유도체

Abstract

PURPOSE: Provided are a 3,4-dihydro-1H-naphthalene derivative as a highly selective cyclooxygenase-2 inhibitor, its pharmaceutically acceptable salt and geometrical isomerism. It improves adverse effects of conventional nonsteroid anti-inflammatory agents, and is useful as a therapeutic agent for inflammational diseases, such as enteritis, peptic ulcer, stomach ulcer, ulcerative colitis, diverticulitis, osteoarthritis, rheumatism, etc. CONSTITUTION: The 3,4-dihydro-1H-naphthalene derivative is represented by the formula(1) or (2), wherein R1 represents methyl or amino; R2 is hydrogen halogen, halogen substituted or nonsubstituted C1-C3-alkyl(methyl, ethyl, etc.), amino, hydroxy, hydroxycarbonyl, nitro or cyano; X represents =D or =S, or represents substituted or unsubstituted =N-OH; A and Q individually represent nitrogen or oxygen atom, wherein nitrogen atom is capable of being substituted with a substituent selected from the group consisting of hydrogen, methyl, ethyl and isopropyl.
본 발명은 사이클로옥시게나제-2에 대한 선택적인 저해활성을 갖는 신규한 하기 화학식 1 또는 2의 3,4-디하이드로-1H-나프탈렌 유도체, 그의 약제학적으로 허용되는 염 및 기하이성체에 관한 것이다: 상기식에서, R 1 , R 2 , X, A 및 Q는 각각 명세서에 정의된 바와 같다.

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