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发明申请
WO0059878A3 INHIBITORS OF LFA-1 BINDING TO ICAMs AND USES THEREOF 审中-公开
LFA-1与ICAM结合的抑制剂及其用途

INHIBITORS OF LFA-1 BINDING TO ICAMs AND USES THEREOF
摘要：
The present invention is directed to compounds that bind to a novel regulatory site in the I domain of LFA-1, and thereby inhibit LFA-1 binding to ICAMs that bind LFA-1. The present invention therefore also provides methods to regulate leukocyte adhesion to endothelial cells. Compounds of the ivnention are useful for the treatment of pathologies, such as those associated inflammatory diseases, autoimmune diseases, tumor metastasis, allograft rejection and reperfusion injury. In particular, the present invention is directed to diaryl sulfides of general structural formula (I), a pharmaceutically acceptable salt, or prodrug thereof, and to the use of diaryl sulfides, and particularly compounds of formula (I), to inhibit LFA-1 binding to an ICAM that binds LFA-1 wherein A and B, independently, are aryl groups selected from the group consisting of 5- and 6-membered aromatic rings, including, but not limited to, phenyl, thienyl, furyl, pyrimidinyl, imidazolyl, pyrazolyl, pyridyl, pyrazinyl, pyrrolyl, and pyridazinyl.
摘要（中）：

本发明涉及与LFA-1的I结构域中的新调节位点结合的化合物，从而抑制LFA-1与结合LFA-1的ICAM结合。 因此，本发明还提供调节白细胞对内皮细胞粘附的方法。 该化合物可用于治疗病理学，例如相关的炎性疾病，自身免疫性疾病，肿瘤转移，同种异体移植排斥和再灌注损伤。 特别地，本发明涉及一般结构式（I）的二芳基硫醚，其药学上可接受的盐或前药，以及使用二芳基硫化物，特别是式（I）化合物抑制LFA-1 与结合LFA-1的ICAM结合，其中A和B独立地是选自5-和6-元芳环的芳基，包括但不限于苯基，噻吩基，呋喃基，嘧啶基，咪唑基 ，吡唑基，吡啶基，吡嗪基，吡咯基和哒嗪基。

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