发明名称 PHENOXYPHENYLHETEROCYCLE DERIVATIVES AS SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRIS).
摘要 The invention provides compounds of general formula (I) wherein R1 is H or C1-C6 alkyl; R2 and R3, together with the interconnecting atoms form a 4 to 8-membered saturated ring containing one or two heteroatoms (including the nitrogen to which R2 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, R or C1-C6alkylthio, and wherein R 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 independen tly selected from oxygen, sulfur and nitrogen; and Z and Y together do not form a fused phenyl ring; R4 and R5, 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, CONR6R7, SO2NR6R7, SO2NHC(=O)R6, OH, C1-4alkoxy, NR8SO2R9, NO2, NR6R11, CN, CO2R10, CHO, SR10, S(O)R9 or SO2R10; 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 R13; wherein R13 is hydroxy, C1-C4alkoxy, F, C1-C6alkyl, haloalkyl, haloalkoxy,-NH2, -NH(C1-C6alkyl) or -N(C1-C6alkyl)2.
申请公布号 MXPA01008860(A) 申请公布日期 2002.08.20
申请号 MX2001PA08860 申请日期 2001.08.30
申请人 PFIZER INC. 发明人 ALAN STOBIE
分类号 A61K31/40;A61P15/00;A61P25/14;A61P25/18;A61P25/24;A61P25/30;A61P43/00;C07D207/08;C07D207/09;C07D207/12;C07D207/20;(IPC1-7):A61K31/40 主分类号 A61K31/40
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