PURPOSE: To obtain the medicine for therapy and prevention of myopia, containing a compound represented by a specified formula, having a relaxation effect on ciliary muscle controlling the crystalline lens, capable of returning the myopia-state refraction properties to the emmetropia state, having a safe and excellent preventive and therapeutic effect on myopia and suitable for eye drops, etc. ;CONSTITUTION: This medicine for therapy and prevention of myopia contains a compound of the formula I [A ring may be substituted; R1 is H, a (protected) amino; R2 is a proton releasing group], especially preferably the compound of the formula II or its salt. In addition, production of this compound is carried out recommendably, e.g. by reacting a compound of formula the III with an active methylene compound (e.g. methyl acetoacetonate) or an acetylenecarboxylic acid derivative (e.g. acetylenedicarboxylic acid dimethyl ester) and subsequently conducting hydrolysis, etc.;COPYRIGHT: (C)1995,JPO
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机译:目的:获得一种用于治疗和预防近视的药物,其包含由指定式表示的化合物,对控制晶状体的睫状肌具有松弛作用,能够使近视状态的屈光特性恢复到正视状态,具有组成:该用于治疗和预防近视的药物含有式I化合物[可以被环取代; R 1 Sub>是H,一个(受保护的)氨基; R 2 Sub>是质子释放基团],特别优选式II的化合物或其盐。另外,该化合物的制备推荐进行,例如,通过气相色谱法。使式Ⅲ化合物与活性亚甲基化合物(如乙酰丙酮甲酯)或乙炔羧酸衍生物(如乙炔二羧酸二甲酯)反应,然后进行水解等; COPYRIGHT:(C)1995,JPO
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