发明名称 BENZOPYRAN, BENZOTHIOPYRAN AND BENZOFURAN DERIVATIVES AS 5-HT4 ANTAGONISTS
摘要 Compounds of formula (I) and pharmaceutically acceptable salts thereof, in which X1-(CH2)x-X2 and the aromatic carbon atoms to which they are attached form a 5-7 membered ring wherein: one of X1 and X2 is O, S or CH2 and the other is CH2; x is 1, 2 or 3; R1 is hydrogen, amino, halo, C1-6 alkyl, hydroxy or C1-6 alkoxy; R2 is hydrogen, halo, C1-6 alkyl, C1-6 alkoxy, nitro, amino or C1-6 alkylthio; R3 is hydrogen, halo, C1-6 alkyl, C1-6 alkoxy or amino; R4 and R5 are independently hydrogen or C1-6 alkyl; Y is O or NH; Z is of sub-formula (a), (b) or (c), wherein n<1> is 1, 2, 3 or 4; n<2> is 1 or 2; n<3> is 2, 3, 4 or 5; q is 0, 1, 2 or 3; p is 0, 1 or 2; m is 0, 1 or 2; Ra is hydrogen or a lipophilic group, such as C1-12 alkyl or aralkyl; or Ra is (CH2) GAMMA R10 wherein r is 2 or 3 and R10 is selected from cyano, hydroxyl, C1-6 alkoxy, phenoxy, C(O)C1-6 alkyl, COC6H5, -CR11R12, NR11COR12, SO2NR11R12 or NR11SO2R12 wherein R11 and R12 are hydrogen or C1-6 alkyl; and R6, R7 and R8 are independently hydrogen or C1-6 alkyl; and R9 is hydrogen or C1-10 alkyl; or a compound of formula (I) wherein the CO-Y linkage is replaced by a heterocyclic bioisostere; and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.
申请公布号 WO9316072(A1) 申请公布日期 1993.08.19
申请号 WO1993GB00214 申请日期 1993.02.01
申请人 SMITHKLINE BEECHAM PLC 发明人 KING, FRANCIS, DAVID;GASTER, LARAMIE, MARY;JOINER, GRAHAM, FRANCIS
分类号 A61K31/443;A61K31/4433;A61K31/445;A61P25/00;A61P25/04;A61P25/20;A61P43/00;C07D405/12;C07D409/12 主分类号 A61K31/443
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