[EN] OPHTHALMIC COMPOSITIONS FOR TREATING OCULAR HYPERTENSION<br/>[FR] COMPOSITIONS OPHTALMIQUES TRAITANT L'HYPERTENSION OCULAIRE
申请人:MERCK & CO INC
公开号:WO2005026128A1
公开(公告)日:2005-03-24
This invention relates to potent potassium channel blocker compounds of Formula (I) or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans, or a pharmaceutically acceptable salt, in vivo hydrolysable ester, enantiomer, diastereomer or mixture thereof: formula (II) represents C6-10 aryl or C3-10 heterocyclyl, said aryl or heterocyclyl optionally substituted with 1-3 groups selected from Ra; Z represents (CH2)nPO(OR)(OR*).
这项发明涉及公式(I)的强效钾通道阻滞剂化合物或其制剂,用于治疗青光眼和其他导致患者眼内压升高的疾病。该发明还涉及利用这些化合物为哺乳动物,特别是人类的眼提供神经保护作用,或其药用可接受的盐、体内可水解酯、对映体、二对映体或其混合物的用途:公式(II)代表C6-10芳基或C3-10杂环烷基,所述芳基或杂环烷基可选择地取代为1-3个Ra基团;Z代表(CH2)nPO(OR)(OR*)。