Alcohols and ethers with aromatic substituents as tachykinin-antagonists
    2.
    发明授权
    Alcohols and ethers with aromatic substituents as tachykinin-antagonists 失效
    具有芳香取代基的醇和醚作为速激肽拮抗剂

    公开(公告)号:US5563161A

    公开(公告)日:1996-10-08

    申请号:US397224

    申请日:1995-03-10

    摘要: Compounds of formula (I), and salt and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; R.sup.1 is H; optionally substituted C.sub.1-6 alkyl; optionally substituted phenyl(C.sub.1-4 alkyl); C.sub.2-6 alkenyl; C.sub.2-6 alkynyl; COR.sup.a ; COOR.sup.a ; COHet; COC.sub.1-6 alkylhalo; COC.sub.1-6 alkylNR.sup.a R.sup.b ; CONR.sup.12 C.sub.1-6 alkylCONR.sup.a R.sup.b ; CONR.sup.a R.sup.b ; or SO.sub.2 R.sup.a ; R.sup.2 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; or R.sup.1 and R.sup.2 together form a chain (CH.sub.2).sub.q optionally substituted by oxo where q is 4 or 5 and where one methylene group may optionally be replaced by an oxygen atom or a group NR.sup.x, where R.sup.x is H or C.sub.1-6 alkyl; R.sup.3 is C.sub.1-3 alkyl substituted by optionally substituted phenyl; R.sup.4 and R.sup.5 are each H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; and Z represents O or S; are tachykinin receptor antagonists useful in therapy.

    摘要翻译: PCT No.PCT / GB93 / 01863 Sec。 371 1995年3月10日 102(e)1995年3月10日PCT PCT 1993年9月3日PCT公布。 第WO94 / 15625号公报 (I)式(I)化合物及其盐和前药,其中Q为任选取代的苯基或二苯甲基; R1是H; 任选取代的C 1-6烷基; 任选取代的苯基(C 1-4烷基); C2-6烯基; C 2-6炔基; COR COORA COHet; COC 1-6烷基卤素; COC 1-6烷基NR a R b; CONR12C1-6烷基CONRaRb; CONRaRb; 或SO2Ra; R 2表示H,C 1-6烷基或C 2-6烯基; 或R 1和R 2一起形成任选被氧代取代的链(CH 2)q,其中q是4或5,并且其中一个亚甲基可以任选地被氧原子或基团NR x取代,其中R x是H或C 1-6烷基; R3是被任意取代的苯基取代的C 1-3烷基; R 4和R 5各自为H,C 1-6烷基或C 2-6烯基; Z表示O或S; 是用于治疗的速激肽受体拮抗剂。