| 摘要 |
Piperidine derivs. of formula (I), their salts and isomers are new. In (I), A1=A2-A3-A4-=CH=CH-CH=CH (gp.(a)), N=CH-CH=CH (gp.(b)), CH=N-CH0CH (gp.(c)), CH=CH-N=CH (gp.(d)) or CH=CH-CH=N (gp(e)); and 1 or 2 H in gps (a)-(e) can be replaced by halo, alkyl, alkoxy, CF3 or OH; R=H, 1-10C alkyl, alkyl substd. by 1 or 2 Ar, gps. 3-6C cycloalkyl or Ar1; R2=H, alkyl, 3-6C cycloalkyl, alkanoyl, alkoxycarbonyl or Ar2- alkyl; L=a gp. (f)-(h) where n=0-2; s=0-6; Alk= alkanediyl; Y=O,S,NR3 or a bond; x=O,S,CHNO2 or NR4; Z=O,S,NR5 or a bond. Het= 5- or 6-membered heterocyclic rinq contg. at least 1N and being condensed with an opt substd. 5- or 6-membered ring; provided that (i) when Het is connected to CsH25 on a C atom then the heterocyclic ring is not condensed with an opt. substd. benzene ring; (ii) when L=(f), (g;Y is not a bond) or (h;Z is not a bond) and Het is connected to CsH25 on an N atom then s is not 0; and (iii) when A1=A2-A3=A4 is (a) or (b) and h is (g;s=0, Y=bond) then Het is other than 2,3-dihydro-2-oxo-1H -benzimidazol-1-yl or 2,3-dihydro-3-oxo- benzoazin-4-yl; R3=H, alkyl, (Ar2) alkyl, 2- alkoxy-1,2-dioxo ethyl or C(X)-R6; R6=H, alkyl, Ar2, Ar2- alkyl, alkoxy, Ar2- alkoxy, mono- or di-( alkyl)amino, NHAr2, Ar2- alkylanino or Ar2- alkyl( alkyl) amino; R4=H, alkyl, CN, NO2, Ar2-sulphonyl, alkylsulphonyl, alkanoyl or Ar2CO; R5=H or alkyl; Ar1=Ar2; thienyl; halothienyl; furanyl ; pyridyl; pyrazinyl; thiazolyl and imidazolyl opt. substd. by alkyl; Ar2=phenyl opt. substd. by 1-3 or halo, OH, NO2, CN, CF3, alkyl, alkoxy, alkylthio, SH, NH2, mono- or di-( alkyl)amino, COOH, alkoxycarbonyl or alkanoyl. - |
