申请人:Elf Sanofi
公开号:US05284838A1
公开(公告)日:1994-02-08
The invention relates to 2,2-dimethylchroman-3-ol derivatives of the formula: ##STR1## in which: A, between N and CO, represents the group --CH.dbd.CH--E.dbd.CH-- or the group ##STR2## Z represents a halogen or a cyano, acetyl, trifluoroacetyl, nitro, alkylthio, carboxyl, phosphono, dial-koxyphosphoryl or alkoxycarbonyl group, the alkylthio and alkoxy groups containing from 1 to 3 carbon atoms; E represents a nitrogen atom or a group C(R.sub.4); R.sub.1 represents hydrogen, a methyl group or a hydroxyl group and R.sub.2 and R.sub.3 each independently represent hydrogen or a methyl group, it being possible for only one of the substituents R.sub.1, R.sub.2 and R.sub.3 to be methyl; and R.sub.4 represents a hydrogen atom, a halogen atom, a methyl group or a hydroxyl group; and to the pharmaceutically acceptable salts of the phosphono or carboxyl group. These derivatives have an antiarrhythmic, antiasthma and antihypertensive activity.
本发明涉及2,2-二甲基色基-3-醇衍生物,其化学式为:##STR1## 其中:A代表N和CO之间的基团,该基团表示为--CH.dbd.CH--E.dbd.CH--或基团##STR2## Z代表卤素或氰基,乙酰基,三氟乙酰基,硝基,烷基硫基,羧基,磷酸酯,二烷氧基磷酰基或烷氧羰基基团,其中烷基硫基和烷氧基团含有1至3个碳原子;E代表氮原子或C(R.sub.4)基团;R.sub.1代表氢,甲基或羟基,R.sub.2和R.sub.3各自独立地代表氢或甲基,其中只有一个取代基R.sub.1,R.sub.2和R.sub.3可以是甲基;R.sub.4代表氢原子,卤素原子,甲基或羟基;以及磷酸酯或羧基团的药学上可接受的盐。这些衍生物具有抗心律失常,抗哮喘和降压活性。