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    • 39. 发明授权
    • 1-aryloxy-2,3,4,5-tetrahydro-3-benzazepines
    • 1-芳氧基-2,3,4,5-四氢-3-苯并吖庚因
    • US4794181A
    • 1988-12-27
    • US819439
    • 1986-01-16
    • Richard C. EfflandJoseph T. KleinLarry Davis
    • Richard C. EfflandJoseph T. KleinLarry Davis
    • C07D223/16
    • C07D223/16
    • The invention relates to 1-aryloxy-2,3,4,5-tetrahydro-3-benzazepines of the formula ##STR1## wherein Y is the same of different and is hydrogen and lower alkoxy; X is hydrogen, halogen, lower alkyl, lower alkoxy, CF.sub.3, NO.sub.2, CN and NH.sub.2 ; R is hydrogen, lower alkyl, cycloalkyllower alkyl, ##STR2## Ar lower alkyl of the formula ##STR3## where Z is hydrogen, lower alkyl, lower alkoxy, halogen CF.sub.3, NO.sub.2 and NH.sub.2 ; Aryloxy lower alkyl of the formula ##STR4## where Z is as previously defined; and an alkylene amine of the formula ##STR5## where R.sub.1 and R.sub.2 are the same or different and are hydrogen and lower alkyl, n is an integer of 1 or 2; and the pharmaceutically acceptable acid addition salts thereof.
    • 本发明涉及式(I)的1-芳氧基-2,3,4,5-四氢-3-苯并吖庚因,其中Y是不同的并且是氢和低级烷氧基; X是氢,卤素,低级烷基,低级烷氧基,CF 3,NO 2,CN和NH 2; R是氢,低级烷基,环烷基低级烷基,其中Z是氢,低级烷基,低级烷氧基,卤素,CF 3,NO 2和NH 2; 其中Z如前所定义的式“IMAGE”的芳氧基低级烷基; 和式“IMAGE”的亚烷基胺,其中R 1和R 2相同或不同,为氢和低级烷基,n为1或2的整数; 及其药学上可接受的酸加成盐。
    • 40. 发明授权
    • 11-substituted 5H,11H-pyrrolo[2,1-c][1,4]benzoxazepines as antipsychotic
and analgesic agents
    • 11-取代的5H,11H-吡咯并[2,1-c] [1,4]苯并氧杂吖庚因作为抗精神病药和镇痛药
    • US4681879A
    • 1987-07-21
    • US713938
    • 1985-03-20
    • Richard C. EfflandLarry DavisKevin J. Kapples
    • Richard C. EfflandLarry DavisKevin J. Kapples
    • C07D401/06C07D498/04C07D413/04A61K31/40A61K31/445
    • C07D401/06
    • There are described novel 11-substituted 5H,11H-pyrrolo[2,1-c][1,4]benzoxazepines of the general formula ##STR1## where m and n are each independently 0, 1 or 2 and m+n is 1 or 2, X and Y are each independently hydrogen, loweralkyl or halogen, and R is hydrogen, cyano, --C(NH.sub.2)NOH, ##STR2## unsubstituted loweralkyl, or substituted loweralkyl having one to three substituents each of which being independently cyano, hydroxy, cycloalkyl of 3-6 carbon atoms, furyl, thienyl, ##STR3## k being 1, 2 or 3, W being each indepentently hydrogen, halogen, hydroxy, loweralkyl, trifluoromethyl, loweralkoxy, nitro, amino, diloweralkylamino, phenoxy, or benzyloxy, and Z being hydrogen, loweralkyl or halogen, which are useful as antipsychotic and analgesic agents; novel intermediate compounds therefor; and methods of synthesizing the foregoing compounds.
    • 描述了通式(IMA)(I)的新颖的11取代的5H,11H-吡咯并[2,1-c] [1,4]苯并氧杂吖庚因,其中m和n各自独立地为0,1或2,m + n为1或2,X和Y各自独立地为氢,低级烷基或卤素,R为氢,氰基,-C(NH 2)NOH,未取代的低级烷基或具有一至三个取代基的取代的低级烷基, 独立地是氰基,羟基,3-6个碳原子的环烷基,呋喃基,噻吩基,1,2或3个,各自独立地为氢,卤素,羟基,低级烷基,三氟甲基, 低级烷氧基,硝基,氨基,二低级烷基氨基,苯氧基或苄氧基,Z为氢,低级烷基或卤素,可用作抗精神病药和镇痛药; 新型中间体化合物; 和上述化合物的合成方法。