公开(公告)号：EP1587781A1

公开(公告)日：2005-10-26

申请号：EP03777543.4

申请日：2003-10-24

申请人： ELI LILLY AND COMPANY

发明人： BOULET, Serge, Louis ,  FILLA, Sandra, Ann ,  GALLAGHER, Peter, Thaddeus ,  HUDZIAK, Kevin, John ,  JOHANSSON, Anette, Margareta ,  KARANJAWALA, Rushad, E. ,  MASTERS, John, Joseph ,  MATASSA, Victor ,  MATHES, Brian, Michael ,  RATHMELL, Richard, Edmund ,  WHATTON, Maria, Ann ,  WOLFE, Chad, Nolan

IPC分类号： C07C217/62 ,  C07C217/64 ,  C07C323/32 ,  C07D275/04 ,  C07D307/86 ,  C07D333/54 ,  C07D333/56 ,  A61K31/381 ,  A61K31/137 ,  A61K31/343 ,  A61K31/425 ,  A61P25/06 ,  A61P25/18 ,  A61P25/24

CPC分类号： C07D275/04 ,  C07C217/16 ,  C07C217/30 ,  C07C217/48 ,  C07C323/32 ,  C07D307/86 ,  C07D333/54 ,  C07D333/62 ,  C07D475/04

摘要： There is provided a compound of formula (I) wherein A is selected from -O- and -S-; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C1-C4 alkyl and C1-C4 alkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C1-C4 alkyl, and C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n- where n is 0, 1 or 2, -CF3, -CN and -CONH2; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n- where n is 0, 1 or 2, nitro, acetyl, -CF3, -SCF3 and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C1-C4 alkyl; Z is selected from OR3 or F, wherein R3 is selected from H, C1-C6 alkyl and phenyl C1-C6 alkyl; R1 and R2 are each independently H or C1-C4 alkyl; and pharmaceutically acceptable salts thereofwith the proviso that when Y is optionally substituted phenyl or optionally substituted 1,3-benzodioxolyl and Z is OR3 and X is optionally substituted phenyl then A is -S-.