申请人:Newron Pharmaceuticals S.p.A.
公开号:EP1524267A1
公开(公告)日:2005-04-20
This invention is related to compounds of general formula I
wherein
Xis oxygen or sulphur or a NR7 group;
R1is C3-C8 alkyl, or C1-C8 alkyl substituted by phenoxy or phenyl, both phenoxy or phenyl being optionally substituted by one or more fluoro, chloro, trifluoromethyl, C1-C6 alkyl, hydroxyl, C1-C6 alkoxy;
R2, R3are independently hydrogen, C1-C6 alkyl, halogen, trifluoromethyl, hydroxy or C1-C6 alkoxy;
R4is hydrogen, C1-C8 alkyl;
R5, R6are independently hydrogen, C1-C3 alkyl, optionally substituted by hydroxy or phenyl;
R7is hydrogen or straight or branched C1-C3 alkyl;
Hetis a five to seven membered, saturated or unsaturated heteromonocyclic or an eight to ten membered, saturated or unsaturated heterobicyclic group, containing one or more heteroatoms chosen independently from nitrogen, oxygen and sulphur, said mono- or bicyclic groups being optionally substituted by C1-C6alkyl, halogen, hydroxyl or C1-C6 alkoxy;
and the pharmaceutically acceptable salts or prodrug thereof, that are active as sodium and/or calcium channel modulators and/or as selective MAO-B inhibitors and therefore useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to, neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urologic, metabolic and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.
本发明涉及一般式I的化合物
其中X是氧或硫或NR7基团;
R1是C3-C8烷基,或C1-C8烷基,被苯氧基或苯基取代,其中苯氧基或苯基可以选配地被一个或多个氟,氯,三氟甲基,C1-C6烷基,羟基,C1-C6烷氧基取代;
R2,R3分别是氢,C1-C6烷基,卤素,三氟甲基,羟基或C1-C6烷氧基;
R4是氢,C1-C8烷基;
R5,R6分别是氢,C1-C3烷基,可以选配地被羟基或苯基取代;
R7是氢或直链或支链C1-C3烷基;
Het是含有一个或多个异原子(独立选择自氮、氧和硫)的五至七元饱和或不饱和杂环或八至十元饱和或不饱和杂双环基团,所述的单环或双环基团可以选配地被C1-C6烷基,卤素,羟基或C1-C6烷氧基取代;
以及药学上可接受的盐或前药,其作为钠和/或钙通道调节剂和/或选择性MAO-B抑制剂具有活性,因此在预防,缓解和治愈广泛的病理学,包括但不限于神经,精神,心血管,炎症,眼科,泌尿学,代谢和胃肠疾病中有用,其中上述机制已被描述为发挥病理作用。