发明名称 Phenoxyphenylheterocyclyl derivatives as SSRIs
摘要 The invention provides compounds of general formula (I) wherein R<1 >is H or C1-C6 alkyl; R<2 >and R<3>, together with the interconnecting atoms form a 4 to 8-membered saturated ring containing one or two heteroatoms (including the nitrogen to which R<2 >is attached) wherein a second heteroatom, if present, is selected from oxygen, nitrogen and sulfur, with the proviso that said ring cannot contain two adjacent heteroatoms; Z is CF3, OCF3, C1-C6alkylthio or C1-C6alkoxy; Y is hydrogen, halogen, -OR<a>, R<a >or C1-C6alkylthio, and wherein R<a >is C1-C4 alkyl optionally substituted with fluorine atoms; or when Z and Y are attached para and meta to the ether linkage linking rings A and B, Z and Y are linked so that, together with the interconnecting atoms, Z and Y form a fused 5 to 7-membered carbocyclic or heterocyclic ring which may be saturated, unsaturated or aromatic, and wherein when Z and Y form a heterocyclic ring, in addition to carbon atoms, the linkage contains one or two heteroatoms independently selected from oxygen, sulfur and nitrogen; and Z and Y together do not form a fused phenyl ring; R<4 >and R<5>, which may be the same or different, are: A-X, wherein A=-CH=CH- or -(CH2)p- where p is 0, 1 or 2; X is hydrogen, F, Cl, Br, I, CONR<6>R<7>, SO2NR<6>R<7>, SO2NHC(=O)R<6>, OH, C1-4alkoxy, NR<8>SO2R<9>, NO2, NR<6>R<11>, CN, CO2R<10>, CHO, SR<10>, S(O)R<9 >or SO2R<10>; or a 5- or 6-membered heterocyclic ring containing 1, 2 or 3 heteroatoms selected from N, S and O, optionally substituted independently by one or more R<13>; wherein R<13 >is hydroxy, C1-C4alkoxy, F, C1-C6alkyl, haloalkyl, haloalkoxy, -NH2, -NH(C1-C6alkyl) or -N(C
申请公布号 US6630504(B2) 申请公布日期 2003.10.07
申请号 US20010939475 申请日期 2001.08.24
申请人 PFIZER INC. 发明人 ANDREWS MARK DAVID;HEPWORTH DAVID;MIDDLETON DONALD STUART;STOBIE ALAN
分类号 A61K31/40;A61P43/00;C07D207/08;C07D207/09;(IPC1-7):A61K31/42;C07D207/02 主分类号 A61K31/40
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