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    • 48. 发明授权
    • Method of using p-acylaminophenoxycarbamates and derivatives as
analgesics
    • 使用对氨基苯氧基氨基甲酸酯和衍生物作为止痛剂的方法
    • US5214061A
    • 1993-05-25
    • US837190
    • 1992-02-18
    • Richard C. AllenRaymond W. Kosley, Jr.Bettina Spahl
    • Richard C. AllenRaymond W. Kosley, Jr.Bettina Spahl
    • C07C271/40C07C271/44C07D213/54C07D521/00
    • C07D231/12C07C271/40C07C271/44C07D213/54C07D233/56C07D249/08
    • This invention relates to p-acylaminophenoxycarbamates having the formula ##STR1## where R.sub.1 and R.sub.2 are each independently hydrogen, loweralkyl, aryl and arylloweralkyl; R.sub.3 is hydrogen, loweralkyl, arylloweralkyl; R.sub.4 is hydrogen, loweralkyl, formyl, alkylcarbonyl, arylloweralkyl, phenylcarbonyl, arylloweralkylcarbonyl, substituted phenylcarbonyl, pyridylcarbonyl, and substituted pyridylcarbonyl with the proviso that if R.sub.4 contains a carbonyl group directly attached to the oxygen of the N-O moiety, R.sub.3 cannot be hydrogen; or R.sub.3 and R.sub.4 taken together from a heterocyclic ring selected from the group consisting of imidazole or loweralkylimidazole; X is hydrogen, halogen, hydroxy, loweralkyl, loweralkoxy, nitro, amino or trifluoromethyl; and p is an integer selected from 0 and 1; the pharmaceutically acceptable acid addition salts thereof, and where applicable, the geometric and stereoisomers and racemic mixtures thereof. The compounds of this invention display utility as analgesics.
    • 本发明涉及具有式“IMAGE”的对酰氨基苯氧基氨基甲酸酯,其中R 1和R 2各自独立地为氢,低级烷基,芳基和芳基低级烷基; R3是氢,低级烷基,芳基低级烷基; R4是氢,低级烷基,甲酰基,烷基羰基,芳基低级烷基,苯基羰基,芳基低级烷基羰基,取代的苯基羰基,吡啶基羰基和取代的吡啶基羰基,条件是如果R4含有直接键合在N-O部分的氧上的羰基,则R3不能是氢; 或者R 3和R 4一起选自咪唑或低级烷基咪唑的杂环; X是氢,卤素,羟基,低级烷基,低级烷氧基,硝基,氨基或三氟甲基; 并且p是选自0和1的整数; 其药学上可接受的酸加成盐,以及适用的几何和立体异构体及其外消旋混合物。 本发明化合物显示出作为止痛剂的效用。