发明名称 HETEROATOM SUBSTITUTED ALKYL BENZYLAMINOQUINUCLIDINES AS SUBSTANCE P ANTAGONISTS
摘要 <p>Compounds useful in the treatment of inflammatory disorders, central nervous system disorders and other disorders of formula (I) and the pharmaceutically-acceptable salts thereof; wherein R is C1-C6 alkyl; X is C1-C6 alkyl having one or more substituents which include at least one heteroatom; Ar?1 and Ar2¿ are each, independently, aryl optionally substituted by one C¿1?-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, halogen, cyano, nitro, phenoxy, mono C1-C6 alkylamino, di C1-C6 alkylamino, halosubstituted C1-C6 alkyl, or halosubstituted C1-C6 alkoxy; Y is hydrogen, C1-C6 akyl, C2-C6 alkenyl, C3-C8 cycloalkyl, Z-(CH2)p-, or W-(CH2)m-CHR?2(CH¿2)n-NR1CO- wherein Y is at the 4-, 5- or 6-position on the quinuclidine ring; R1 is hydrogen, C¿1?-C6 alkyl, benzyl or -(CH2)r-W; R?2¿ is hydrogen or C¿1?-C6 alkyl which may be substituted by one hydroxy, amino, methylthio, methylmercapto, benzyl, 4-hydroxybenzyl, 3-indolylmethyl or -(CH2)r-W; R?1¿ may form a ring with R2; Z is C¿1?-C6 alkoxy, -CONR?4R5, -CO¿2R?4, -CHR4OR5, -CHR4NR5R6, -COR4, -CONR4OR5¿ or optionally substituted aryl; each W is independently cyano, hydroxymethyl, C¿2?-C6 alkoxymethyl, aminomethyl, mono C1-C6 alkylaminomethyl, di C1-C6 alkylaminomethyl, carboxyl, carbamoyl or C1-C6 alkoxycarbonyl; R?4, R5 and R6¿ are independently hydrogen, C¿1?-C6 alkyl, C1-C6 alkoxy, C3-C8 cycloalkyl or an optionally substituted aryl or heterocyclic group; p is 0 to 6; and m, n and r are each, independently, 0 to 3.</p>
申请公布号 WO1994026740(A1) 申请公布日期 1994.11.24
申请号 JP1994000781 申请日期 1994.05.13
申请人 发明人
分类号 主分类号
代理机构 代理人
主权项
地址