申请人:——
公开号:US20020013318A1
公开(公告)日:2002-01-31
The present invention describes pyridazinone compounds of formula I
1
which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2). COX-2 is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1) which is an important “housekeeping” enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectivity of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently marketed non-steroidal anti-inflammatory drugs (NSAIDs).
本发明描述了一类式I1的吡啶嗪化合物,它们是环氧合酶(COX)抑制剂,特别是选择性抑制剂环氧合酶-2(COX-2)。COX-2是与炎症相关的可诱导异构体,而不是重要的“家政”酶在许多组织中,包括胃肠道(GI)和肾脏中的构成性异构体环氧合酶-1(COX-1)。这些化合物对COX-2的选择性最小化了目前市场上非甾体抗炎药(NSAIDs)所见到的不良的GI和肾脏副作用。