申请人:Merck & Co., Inc.
公开号:US05646000A1
公开(公告)日:1997-07-08
The invention is directed to a series of novel compounds, and their pharmaceutically acceptable salts, of the formula ##STR1## wherein R is C.sub.0-6 alkyl substituted with R.sup.5 or a mono or polycyclic aromatic or heteroaromatic system comprised of 5 or 6-membered aromatic or heteroaromatic rings that are either unsubstituted or substituted with one or more of R.sup.1 and R.sup.2 ; R.sup.1 and R.sup.2 are independently C.sub.1-6 alkyl, carboxyl, hydroxyl, azido, nitro, amino, C.sub.1-6 alkylamino, C.sub.1-6 dialkylamino, arylamino, aryl C.sub.1-6 alkylamino, hydroxysulfonyl or arylazo; aryl is a phenyl or naphthyl ring which is unsubstituted or substituted with one or more of R.sup.3 and R.sup.4 ; R.sup.3 and R.sup.4 are independently C.sub.1-6 alkyl, azido, nitro, amino, C.sub.1-6 dialkylamino or hydroxysulfonyl; R.sup.5 is ##STR2## provided that when R is an unsubstituted monocyclic ring, the monocyclic ring is not phenyl or pyridyl. Such compounds are useful as fluorescent probes for identifying antiplatelet agents which selectively bind to activated platelets.
该发明涉及一系列新颖化合物及其药用可接受的盐,其化学式为##STR1##其中R是C.sub.0-6烷基,被R.sup.5取代,或者是一个由5个或6个芳香环或杂芳环组成的单环或多环芳香体系,这些环要么未取代,要么被一个或多个R.sup.1和R.sup.2取代;R.sup.1和R.sup.2独立地是C.sub.1-6烷基,羧基,羟基,叠氮基,硝基,氨基,C.sub.1-6烷基氨基,C.sub.1-6二烷基氨基,芳基氨基,芳基C.sub.1-6烷基氨基,羟基磺酰基或芳基偶氮基;芳基是一个未取代或被一个或多个R.sup.3和R.sup.4取代的苯环或萘环;R.sup.3和R.sup.4独立地是C.sub.1-6烷基,叠氮基,硝基,氨基,C.sub.1-6二烷基氨基或羟基磺酰基;R.sup.5是##STR2##但是当R是一个未取代的单环时,该单环不是苯基或吡啶基。这些化合物可用作荧光探针,用于鉴定选择性结合到活化血小板的抗血小板药物。