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3-Phenylureido-azepin-2-one and 3-PHENYLUREIDO-AZEPIN-2-ONES USEFUL AS CHOLECYSTOKININ ANTAGONISTS, which are useful as cholecystokinin antagonists,
3-Phenylureido-azepin-2-one and 3-PHENYLUREIDO-AZEPIN-2-ONES USEFUL AS CHOLECYSTOKININ ANTAGONISTS, which are useful as cholecystokinin antagonists,
The present invention relates to novel substituted hexahydroazepinones and tetrahydrobenzazepinones of the general formulas (I) and (II), and novel intermediates used in the synthesis of these compounds:;In the above formula, YOneAnd Y2Is independently phenyl, thienyl, pyridyl, furyl, pyrimidyl, (C3-C8) Straight or branched chain alkyl and (C3-C8Cycloalkyl, wherein said phenyl, thienyl, pyridyl, furyl and pyrimidyl are optionally substituted with halo (such as chloro, fluoro, bromo or iodo), (COne-C6) Alkyl, (COne-C6) Alkoxy, nitro, amino and trifluoromethyl, said cycloalkyl being optionally substituted with one or two substituents independently selected from the group consisting of (COne-C6) Alkyl; /RTI ZOneAnd Z2Is independently halo, (COne-C6) Alkyl, (COne-C6) Thioalkyl, (COne-C6) Alkoxy, trifluoromethyl, (COne-C6) Carboalkoxy, amino, and nitro; ROneIs phenyl, CO2R2, S02NR3R6Or CONR4R5, Wherein said phenyl is optionally substituted with halo, (COne-C6) Alkyl, (COne-C6) Optionally substituted with one or two substituents independently selected from the group consisting of alkoxy, nitro, amino and trifluoromethyl, R2, R3, R4, R5And R6Is independently hydrogen, (C3-C12) Alkyl and a condensed saturated carbocyclic system containing two or three rings.;These compounds are useful for the treatment and prevention of gastrointestinal diseases, pain and anxiety disorders.
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机译:本发明涉及通式(I)和(II)的新型取代的六氢a庚酮和四氢苯并ze庚酮,以及用于合成这些化合物的新型中间体:上式中,Y 和Y 2 Sup>分别为苯基,噻吩基,吡啶基,呋喃基,嘧啶基,(C 3 Sub> -C 8 Sub>)直链或支链烷基和(C < Sub> 3 Sub> -C 8 Sub>环烷基,其中所述苯基,噻吩基,吡啶基,呋喃基和嘧啶基任选地被卤素(例如氯,氟,溴或碘)取代,(C < Sub>一个 Sub> -C 6 Sub>)烷基,(C 一个 Sub> -C 6 Sub>)烷氧基,硝基,氨基和三氟甲基,环烷基任选地被一个或两个独立地选自(C One Sub> -C 6 Sub>)烷基,Z 1 sub>的取代基取代Sup>和Z 2 Sup>独立地是(C One Sub> -C 6 Sub>)烷基,(C One Sub>- C 6 Sub>)硫代烷基,(C One Su b> -C 6 Sub>)烷氧基,三氟甲基,(C One Sub> -C 6 Sub>)烷氧基,氨基和硝基; R 1 Sup>是苯基,CO 2 Sup> R 2 Sup>,S0 2 Sup> NR 3 Sup> R 6 Sup>或CONR 4 Sup> R 5 Sup>,其中所述苯基任选地被卤素取代,(C 一个 Sub> -C < Sub> 6 Sub>)烷基,(C 一个 Sub> -C 6 Sub>)任选地被一个或两个独立地选自烷氧基,硝基,氨基的取代基取代和三氟甲基,R 2 Sup>,R 3 Sup>,R 4 Sup>,R 5 Sup>和R 6 Sup>独立地为氢,(C 3 Sub> -C 12 Sub>)烷基和含有两个或三个环的稠合饱和碳环系统;这些化合物可用于治疗和预防胃肠道疾病,疼痛和焦虑症。
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