申请人:Kyowa Hakko Kogyo Co., Ltd.
公开号:US05703085A1
公开(公告)日:1997-12-30
The present invention relates to novel xanthine derivatives and pharmaceutically acceptable salts thereof, represented by Formula (I): ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 independently represent hydrogen, lower alkyl, lower alkenyl, or lower alkynyl, R.sup.4 represents lower alkyl, or substituted or unsubstituted aryl, R.sup.5 and R.sup.6 independently represent hydrogen, lower alkyl, and lower alkoxy, or R.sup.5 and R.sup.6 are combined together to represent --O--(CH.sub.2)p--O-- (p is an integer of 1 to 3), n represents 0, 1, or 2, and m represents 1 or 2. The compounds of the present invention have an adenosine A.sub.2 receptor antagonistic activity, and are useful for the treatment or prevention of various kinds of diseases caused by hyperergasia of adenosine A.sub.2 receptors (for example, Parkinson's disease, senile dementia, depression, asthma, and osteoporosis).
本发明涉及新型黄嘌呤衍生物及其药学上可接受的盐,其化学式表示为(I):##STR1## 其中,R.sup.1、R.sup.2和R.sup.3独立地表示氢、低级烷基、低级烯基或低级炔基,R.sup.4表示低级烷基或取代或未取代的芳基,R.sup.5和R.sup.6独立地表示氢、低级烷基和低级烷氧基,或者R.sup.5和R.sup.6结合在一起表示--O--(CH.sub.2)p--O-- (p为1至3的整数),n表示0、1或2,m表示1或2。本发明的化合物具有腺苷A.sub.2受体拮抗活性,可用于治疗或预防由腺苷A.sub.2受体高度兴奋引起的各种疾病(例如帕金森病、老年性痴呆、抑郁症、哮喘和骨质疏松症)。