| 摘要 |
<p>PURPOSE:To provide the subject new carbostyril derivatives excellent in thromboxane A2 antagonism, useful for treatment and prevention of diseases and symptoms caused by thromboxane A2, e.g. thrombosis, vasospasm and asthma and excellent in safety. CONSTITUTION:Compounds of formula I (R<1> is H or a lower alkyl; R<2> and R<3> are H, OH, a lower alkyl or together form CO; X is H or a halogen; Y is CH2COOH or OCH2COOH; Formula II is a single bond or a double bond) or their pharmaceutically permissible salts e.g. {5-[2-(4- chlorobenzenesulfonylamino)ethyl]carbostyril-8-yl]oxyacetic acid} of formula III. In case of Y=OCH2COOH, the above-mentioned compound can be produced by four steps from a compound of formula IV (Bz is benzyl) (through compounds of formulae V to VII (tBu is t-butyl; R<4> is a lower alkyl). In addition, the dosage of the compound of formula I required for improving or preventing the above- mentioned diseases is generally 1 to 1000mg, preferably 5 to 500mg per day per an adult in oral administration.</p> |
