发明名称 POSITIVE MODULATORS OF NICOTINIC RECEPTOR AGONISTS
摘要 A compound of formula (I) wherein R<1a>, R<1b>, R<3a> and R<3b> independently represent hydrogen or C1-C4 alkyl; R<2a> and R<2b> independently represents hydrogen, C1-C4 alkyl or CH2CN; A<1> represents O, S or NR<4a>; B<1> represents O, S or NR<4b>; R<4a> represents hydrogen, C1-C4 alkyl, C2-C4 alkenyl; or together R<3a> and R<4a> form a ring; R<4b> represents hydrogen, C1-C4 alkyl, C2-C4 alkenyl; or together R<3b> and R<4b> form a ring; A<2> and B<2> independently represent C(O), C(NH), OC(O), NHC(O), NHC(S), SO2, or a bond; Z represents (CH2)n Y(CH2)m; n and m are independently 0-4; Y represents O, S, NR<5>, CHR<6>, Ar, or Ccy; Ccy represents a 5-10 membered carbocycle including cyclopentane and adamantane; Ar represents phenyl, naphthyl; or a 5- or 6- membered heterocyclic ring containing zero to four nitrogens, zero to one sulfurs and zero to one oxygens; Ar is optionally substituted with one or more substituents selected from: hydrogen, halogen, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, CN, NO2, CF3, OR<7>, NR<8>R<9>, and COOR<10>; R<7>, R<8> and R<9> are independently hydrogen, C1-C4 alkyl, aryl, heteroaryl, C(O)R<11>, C(O)R<12>, SO2R<13>, or; R<8> and R<9> together may be (CH2)j Q(CH2)k, where Q is O, S, NR<14> or a bond; j is 2-4; k is 0-2; R<5>, R<6>, R<10>, R<11>, R<12>, R<13> and R<14> are independently hydrogen, C1-4 alkyl, aryl or heteroaryl; or an enantiomer thereof, and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially for treatment of conditions associated with reductions in nicotinic transmission. The compounds of the invention enhance the efficacy of agonists at nicotinic receptors.
申请公布号 WO0132620(A1) 申请公布日期 2001.05.10
申请号 WO2000SE02149 申请日期 2000.11.01
申请人 ASTRAZENECA AB;BALESTRA, MICHAEL;GURLEY, DAVID;ROSAMOND, JAMES 发明人 BALESTRA, MICHAEL;GURLEY, DAVID;ROSAMOND, JAMES
分类号 A61K45/00;A61K31/404;A61K45/06;A61P1/00;A61P25/00;A61P25/04;A61P25/16;A61P25/18;A61P25/22;A61P25/24;A61P25/28;A61P25/34;A61P43/00;C07D209/08;(IPC1-7):C07D209/08 主分类号 A61K45/00
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