Process for preparing varenicline, varenicline intermediates, pharmaceutically acceptable salts thereof
    6.
    发明授权
    Process for preparing varenicline, varenicline intermediates, pharmaceutically acceptable salts thereof 失效
    伐伦碱,伐伦碱中间体及其药学上可接受的盐的制备方法

    公开(公告)号:US08314235B2

    公开(公告)日:2012-11-20

    申请号:US13060755

    申请日:2009-08-31

    IPC分类号: C07D241/40

    CPC分类号: C07D471/08

    摘要: Provided herein is an improved, convenient, commercially viable and environmentally friendly process for the preparation of varenicline or a pharmaceutically acceptable salt thereof comprising reacting 1-(4,5-diamino-10-aza-tricyclo[6.3.1.02 7]dodeca-2(7),3,5-trien-10-yl)-2,2,2-trifluoro-ethanone with chloroacetaldehyde in the presence of an oxygen source. Provided further herein is an improved and industrially advantageous process for the preparation of 1-(4,5-diamino-10-aza-tricyclo[6.3.1.02 7]dodeca-2(7),3,5-trien-10-yl)-2,2,2-trifluoro-ethanone.

    摘要翻译: 本文提供了一种改进的,方便的,商业上可行的和环境友好的伐伦碱或其药学上可接受的盐的制备方法,其包括使1-(4,5-二氨基-10-氮杂 - 三环[6.3.1.02 7]十二碳-2 (7),3,5-三烯-10-基)-2,2,2-三氟乙酮与氯乙醛在氧源的存在下反应。 本文进一步提供了一种改进和工业上有利的制备1-(4,5-二氨基-10-氮杂 - 三环[6.3.1.02 7]十二-2(7),3,5-三烯-10-基 )-2,2,2-三氟乙酮。

    1,2,3,6-tetrahydropyrimidine-2-one compositions, articles and therapeutic methods for upper airway breathing disorders
    10.
    发明授权
    1,2,3,6-tetrahydropyrimidine-2-one compositions, articles and therapeutic methods for upper airway breathing disorders 失效
    1,2,3,6-四氢嘧啶-2-酮组合物,用于上呼吸道呼吸障碍的制品和治疗方法

    公开(公告)号:US06933301B2

    公开(公告)日:2005-08-23

    申请号:US10267896

    申请日:2002-10-08

    申请人: Edward T. Wei

    发明人: Edward T. Wei

    摘要: A therapeutic composition is provided that comprises a 1-R1-phenyl, 4-R2-phenyl substituted 1,2,3,6-tetrahydropyrimidine-2-one cold receptor agonist in a therapeutically effective amount. The cold receptor agonist may be represented by the general formula 1-[R1-phenyl]-4-[R2-phenyl]-1,2,3,6-tetrahydropyrimidine-2-one wherein: R1 is -hydroxy, -chloro, -fluoro, -alkyl, -acetoxy, -trifluoromethyl; and R2 is -nitro, -chloro, -fluoro, -alkyl, -trifluoromethyl. Therapeutic compositions of the invention when formulated for delivery to the mucous membranes of the nose and throat alleviate the sensations of airway obstruction and provide symptomatic relief of upper airway breathing disorders.

    摘要翻译: 提供治疗组合物,其包含治疗有效量的1-R 1 - 苯基,4-R 2 - 苯基取代的1,2,3,6-四氢嘧啶-2-酮冷受体激动剂。 冷受体激动剂可以由通式1- [R 1 - 苯基] -4- [R 2 - 苯基] -1,2,3,6-四氢嘧啶-2-酮表示,其中:R1是 - 羟基, - 氯, - 氟, - 烷基, - 乙酰氧基, - 三氟甲基; 并且R 2是 - 硝基, - 氯, - 氟, - 烷基, - 三氟甲基。 当配制用于输送到鼻和喉部的粘膜时,本发明的治疗组合物减轻气道阻塞的感觉并提供上呼吸道呼吸障碍的症状缓解。