An adenosine A2a receptor antagonist compound, pharmaceutical composition comprising the same, the use thereof and processes for the preparation of intermediate compounds
Bernard R. Neustadt,Craig D. Boyle,Deen Tulshian,Lisa S. Silverman,Neil A. Lindo,Samuel Chackalamannil,William J. Greenlee,Yan Xia
申请号：
BRPI0111015
公开号：
BRPI0111015B1
申请日:
2001.05.24
申请国别(地区):
BR
年份:
2017
代理人:
摘要：
"adenosine α-2α receptor antagonists". compounds having the formula (i) or a pharmaceutically acceptable salt thereof, wherein r is optionally substituted phenyl, cycloalkenyl or heteroaryl； x is alkylene or -C (o) ch 2 - -； y is -n (r ^ 2 ^) ch ~ 2 ~ ch ~ 2 ~ n (r ^ 3 ^) -, - och ~ 2 ~ ch ~ 2 ~ n (r ^ 2 ^) -, - o-, - s-, -ch ~ 2-s-, (ch ~ 2 ~) ~ 2 -nh-, or optionally substituted, (ia), m and n are 2 or 3, and q is optionally substituted nitrogen or carbon； ez is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R 6 6 -c (o) -, r 6 6 -so-2 -, r 6 6 -oc (o) -, r 7 7 - n (r ^ 8 ^) - c (o) -, r ^ 7 ^ n (r ^ 8 ^) - c (s) -, phenyl-ch (oh) -, or phenyl-c (= nor ^ 2 ^ ) -； or when q is ch, (ib), phenylamino or pyridylamino； or z and y together are substituted piperidinyl or substituted phenyl； er ^ 2 ^, r ^ 3 ^, r ^ 6 ^, r ^ 7 ^, and r ^ 8 ^ are as defined in the application are disclosed, their use in the treatment of parkinson's disease alone or in combination with other agents for treatment of parkinson's disease, and pharmaceutical compositions comprising them； Also disclosed are processes for the preparation of intermediates useful for the preparation of the compounds of formula (I)."antagonistas de receptor a~ 2a~ de adenosina". compostos tendo a fórmula estrutural (i) ou um sal farmaceuticamente aceitável do mesmo, em que r é fenila, cicloalquenila ou heteroarila opcionalmente substituído； x é alquileno ou -c(o)ch~ 2~-； y é -n(r^ 2^) ch~ 2~ch~ 2~n(r^ 3^)-,-och~ 2~ch~ 2~n(r^ 2^)-,-o-, -s-, -ch~ 2~s-, (ch~ 2~)~ 2~-nh-, ou opcionalmente substituído, (ia), m e n são 2 ou 3, e q é nitrogênio ou carbono opcionalmente substituído； e z é fenila, fenilalquila ou heteroarila opcionalmente substituído, difenilmetila, r^ 6^-c(o)-, r^ 6^-so~ 2~-, r^ 6^-oc(o)-, r^ 7^-n(r^ 8^)-c(o)- , r^ 7^n(r^ 8^)-c(s)-, fenil-ch(oh)-, ou fenil-c(=nor^ 2^)-； ou quando q é ch, (ib), fenilamino ou piridilamino； ou z e y juntos são piperidinila substituída ou fenila substitu
