申请人:Whitby Research Incorporated
公开号:EP0257285A2
公开(公告)日:1988-03-02
This invention provides a method for reducing the intraocular pressure in mammals which comprises administering an effective amount of a compound selected from the group consisting of compounds represented by the general formula:
where R₂, R₃ and R₄ are each selected from the group consisting of H and OA; A is H or is selected from the group consisting of hydrocarbyl radicals, e.g. lower alkyl radicals, i.e. methyl, ethyl, propyl etc., or --R₅,
wherein R₅ is selected from the group consisting of hydrocarbyl radicals, e.g. alkyl and aromatic residues; n is 2 or 3; and R₁ is selected from the group consisting phenyl and substituted phenyl, e.g. phenyl substituted with hydroxy, nitro, azido, sulfate, sulfonamido, halogen, hydrocarbyl and hetero atom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12 carbon atoms, with the proviso that at least one of R₂, R₃ and R₄ is H, that at least one of R₂, R₃ and R is not H and that R₂ and R₄ are not both OA; and pharmaceutically-acceptable salts thereof, in an ophthalmic carrier. Preferably, R is phenyl or 3 or 4 hydroxyphenyl.
本发明提供了一种降低哺乳动物眼内压的方法,该方法包括施用有效量的选自通式 所示化合物组成的组的化合物:
其中 R₂、R₃和 R₄各自选自由 H 和 OA 组成的组;A 为 H 或选自由烃基,例如低级烷基,即甲基、乙基、丙基等,或--R₅组成的组、
其中,R₅ 选自由烃基(如烷基和芳香残基)组成的组;n 为 2 或 3;R₁ 选自由苯基和取代苯基(如被羟基取代的苯基)组成的组。被羟基、硝基、叠氮基、硫酸基、磺酰胺基、卤素基、烃基和杂原子取代的烃基取代的苯基,其中所述杂原子选自由卤素、氮、氧、硫和磷组成的组、R₂、R₃ 和 R₄ 中至少有一个是 H,R₂、R₃ 和 R 中至少有一个不是 H,R₂ 和 R₄ 不是都是 OA;及其在眼科载体中的药学上可接受的盐类。最好 R 是苯基或 3 或 4 羟基苯基。