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    • 9. 发明授权
    • Hetercyclic compounds, processes for their preparation and
pharmaceutical compositions containing them
    • 异环化合物,其制备方法和含有它们的药物组合物
    • US5328927A
    • 1994-07-12
    • US021826
    • 1993-02-24
    • Richard T. LewisKevin J. MerchantAngus M. MacLeod
    • Richard T. LewisKevin J. MerchantAngus M. MacLeod
    • C07D333/60A61K31/34A61K31/38A61K31/381A61K31/40A61K31/403A61K31/404A61P43/00C07C237/22C07C239/08C07C251/40C07C255/24C07C255/30C07C317/28C07C323/24C07D209/14C07D209/16C07D307/81C07D333/58C07K1/113C07K5/02A61K31/405C07D209/10
    • C07D333/58C07D209/16
    • Compounds of formula (I), and salts and prodrugs thereof ##STR1## wherein Q.sup.1 is halo substituted phenyl; naphthyl; indolyl; benzthiophenyl; benzofuranyl; benzyl; or fluorenyl; . . is an optional covalent bond;one of X and Y is H and the other is hydroxy or C.sub.1-6 alkoxy, or X and Y are together .dbd.0 or .dbd.NOR.sup.5 ;R.sup.1 and R.sup.2 are H; C.sub.1-6 alkyl optionally substituted by hydroxy, cyano, COR.sup.c, CO.sub.2 R.sup.c, CONR.sup.c R.sup.d, or NR.sup.c R.sup.d (where R.sup.c and R.sup.d are H, C.sub.1-6 alkyl or phenyl(C.sub.0-4 alkyl) optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halo and trifluoromethyl); phenyl(C.sub.1-4 alkyl) (optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halo or trifluoromethyl); COR.sup.c ; CO.sub.2 R.sup.c ; CONR.sup.c R.sup.d ; COC.sub.1-6 alkylNR.sup.c R.sup.d ; CONR.sup.c COOR.sup.d ; or SO.sub.2 R.sup.c ;R.sup.3 is H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; andR.sup.4 is phenyl optionally substituted by C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, OR.sup.a, SR.sup.a, SOR.sup.a, NR.sup.a R.sup.b, NR.sup.a COR.sup.b, NR.sup.a CO.sub.2 R.sup.b, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b, where R.sup.a and R.sup.b are H, C.sub.1-6 alkyl, phenyl or trifluoromethyl; are tachykinin antagonists.
    • 式(I)化合物及其盐和前药其中Q 1是卤素取代的苯基; 萘基; 吲哚基 苯硫酚 苯并呋喃基 苄基; 或芴基; 。 。 。 是可选的共价键; X和Y之一是H,另一个是羟基或C 1-6烷氧基,或X和Y一起= 0或= NOR5; R1和R2是H; 任选被羟基,氰基,CORc,CO2Rc,CONRcRd或NRcRd取代的C 1-6烷基(其中R c和R d为H,任选被C 1-6烷基,C 1-6烷氧基,卤素和三氟甲基取代的C 1-6烷基或苯基(C 0-4烷基) ); 苯基(C 1-4烷基)(任选被C 1-6烷基,C 1-6烷氧基,卤素或三氟甲基取代); CORC; CO2Rc; CONRcRd; COC 1-6烷基NR c R d; CONRcCOORd; 或SO2Rc; R3是H,C1-6烷基或C2-6烯基; R4是任选被C 1-6烷基,C 2-6烯基,C 2-6炔基,卤素,氰基,硝基,三氟甲基,三甲基甲硅烷基,OR a,SR a,SOR a,NR a R b,NR a COR b,NR a CO 2 R b,CO 2 R a或CONR a R b任意取代的苯基,其中R a和R b是 H,C 1-6烷基,苯基或三氟甲基; 速激肽拮抗剂。