发明名称 HETEROATOM SUBSTITUTED ALKYL BENZYLAMINOQUINUCLIDINES AS SUBSTANCE P ANTAGONISTS
摘要 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 Ar<2> are each, independently, aryl optionally substituted by one C1-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>(CH2)n-NR<1>CO- wherein Y is at the 4-, 5- or 6-position on the quinuclidine ring; R<1> is hydrogen, C1-C6 alkyl, benzyl or -(CH2)r-W; R<2> is hydrogen or C1-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 R<2>; Z is C1-C6 alkoxy, -CONR<4>R<5>, -CO2R<4>, -CHR<4>OR<5>, -CHR<4>NR<5>R<6>, -COR<4>, -CONR<4>OR<5> or optionally substituted aryl; each W is independently cyano, hydroxymethyl, C2-C6 alkoxymethyl, aminomethyl, mono C1-C6 alkylaminomethyl, di C1-C6 alkylaminomethyl, carboxyl, carbamoyl or C1-C6 alkoxycarbonyl; R<4>, R<5> and R<6> are independently hydrogen, C1-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.
申请公布号 WO9426740(A1) 申请公布日期 1994.11.24
申请号 WO1994JP00781 申请日期 1994.05.13
申请人 PFIZER PHARMACEUTICALS INC.;PFIZER INC.;SATAKE, KUNIO 发明人 SATAKE, KUNIO
分类号 A61K31/435;A61P1/00;A61P11/00;A61P25/00;A61P25/04;A61P25/06;A61P29/00;C07D453/02;(IPC1-7):C07D453/02 主分类号 A61K31/435
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