NEUSTADT BERNARD R.,LINDO NEIL A.,GREENLEE WILLIAM J.,TULSHIAN DEEN,SILVERMAN LISA S.,XIA YAN,BOYLE CRAIG D.,CHACKALAMANNIL SAMUEL
申请号:
CZ20023886
公开号:
CZ303790B6
申请日:
2001.05.24
申请国别(地区):
CZ
年份:
2013
代理人:
摘要:
Deriváty pyrimidinu obecného vzorce I nebo jejich farmaceuticky prijatelná sul, kde R je poprípade substituovaný fenyl, cykloalkenyl nebo heteroaryl; X je alkylen nebo -C(O)CH.sub.2.n.-; Y je poprípade substituovaná skupina (Ia), m a n jsou 2 az 3, Q je atom dusíku nebo poprípade substituovaný atom uhlíku; a Z je poprípade substituovaný fenyl, fenylalkyl nebo heteroaryl, difenylmethyl, R.sup.6.n.-C(O)-, R.sup.6.n.-SO.sub.2.n.-, R.sup.6.n.-OC(O)-, R.sup.7.n.-N(R.sup.8.n.)-C(O)-, R.sup.7.n.-N(R.sup.8.n.)-C(S)-, fenyl-CH(OH)-, nebo fenyl-C(=NOR.sup.2.n.)-; nebo jestlize Q je CH, (Ib), fenylamino nebo pyridylamino; nebo Z a Y spolu tvorí substituovaný piperidinyl nebo substituovaný fenyl; a R.sup.2.n., R.sup.3.n., R.sup.6.n., R.sup.7 .n.a R.sup.8 .n.mají specifické významy, jejich pouzití pri lécení Parkinsonovy choroby samostatne nebo v kombinaci s jinými prostredky pro lécení Parkinsonovy choroby, a farmaceutické prostredky s jejich obsahem.In the present invention, there are disclosed pyrimidine derivatives of the general formula I or pharmaceutically acceptable salt thereof, wherein R represents optionally substituted phenyl, cycloalkenyl, or heteroaryl; X denotes alkylene or -C(O)CHi2-; Y represents an optionally substituted group (Ia), m and n are 2 to 3, and Q denotes a nitrogen atom or optionally a substituted carbon atom; and Z denotes an optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, Re6-C(O)-, Re6-SOi2-, Re6-OC(O)-, Re7-N(Re8)-C(O)-, Re7-N(Re8)-C(S)-, phenyl-CH(OH)-, or phenyl-C(=NORe2)-; or when Q represents CH, (Ib), phenylamino or pyridylamino; or Z and Y together denote substituted piperidinyl or substituted phenyl; and Re2, Re3, Re6, Re7, and Re8 are as defined in the specification, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.