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Tetrahydropyran derivatives as antagonists of Neurokinin 1 receptor (nk-1)

机译:四氢吡喃衍生物作为Neurokinin 1受体(nk-1)的拮抗剂

摘要

Refers to a compound of formula I wherein R1 IS F, trifluoromethyl; R2 IS F, trifluoromethyl; R3 is Methyl or hydroxymethyl; R4 is Halogen, Hydroxy, alquelino c2-c4, alquinilo c2-c4, N3, nr5r6,Among others, R5 is H, c1-c4 alkyl, cycloalkyl C3 - C7, cicloalquil C3 - C7 (c1-c4 alkyl, alkyl c2-c4, among others; R6 h, c1-c4 alkyl, cycloalkyl alkyl C2 C3 - C7, C4,Among others, R5 or R6 together to form a ring heteroalifatico 4 to 7 Atoms Ring; Z is a Link, alquileno cicloalquileno C1 - C6 C3, C6, among others, N is 1 - 2, p is 1 - 2; Q is 1 - 2.Preferred compounds are CIS, trans - (2R, 3S, 4R, 8R) - 2 - [1 - (3,5-bis (trifluoromethyl) phenyl) ethoxy] - 3 - (3,4-difluorophenyl) - 4 - viniltetrahidropirano, trans, trans - (2R, 3S, 4S, 8R) - 2 - [1 - (3),5 - bis (trifluoromethyl) phenyl) ethoxy] - 3 - (3,4-difluorophenyl) - 4 - viniltetrahidropirano, 2R, 3S, 4R, 8R) - 2 - [1 - (3,5-bis (trifluoromethyl) phenyl) ethoxy] - 3 - (3,4-difluorophenyl) - 4 - carbaldehido tetrahydropyran,Among others. These compounds are antagonists of Neurokinin 1 receptor (nk-1) and are useful for the treatment of disorders of the central nervous system
机译:指式I化合物,其中R 1为F,三氟甲基; R 2 IS F,三氟甲基; R3是甲基或羟甲基; R 4是卤素,羟基,alquelino c2-c4,alquinilo c2-c4,N3,nr5r6等,R5是H,c1-c4烷基,环烷基C3-C7,环氯基C3-C7(c1-c4烷基,c2-c4烷基C4,尤其是; R6h,c1-c4烷基,环烷基C2 C3-C7,C4,R5或R6等一起形成环杂芳基4至7个原子环; Z是连接基,alquileno cicloalquileno C1-C6 C3,C6等,N为1-2,p为1-2; Q为1-2。首选化合物为CIS,反式-(2R,3S,4R,8R)-2-[1-(3, 5-双(三氟甲基)苯基乙氧基]-3-(3,4-二氟苯基)-4-viniltetrahidropirano,反式,反式-(2R,3S,4S,8R)-2-[1-(3),5-双(三氟甲基)苯基乙氧基]-3-(3,4-二氟苯基)-4-viniltetrahidropirano,2R,3S,4R,8R)-2-[1--(3,5-双(三氟甲基)苯基)乙氧基] -3-(3,4-二氟苯基)-4-羰基四氢吡喃,除其他外。这些化合物是Neurokinin 1受体(nk-1)的拮抗剂,可用于治疗中枢神经系统疾病

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