Retro-anandamides, high affinity and stability cannabinoid receptor ligands
    4.
    发明授权
    Retro-anandamides, high affinity and stability cannabinoid receptor ligands 有权
    复方昂丹酰胺,高亲和力和稳定性大麻素受体配体

    公开(公告)号:US07276613B1

    公开(公告)日:2007-10-02

    申请号:US10110862

    申请日:2000-10-18

    Abstract: Novel retro-anandamides are presented which have high affinities for the cannabinoid CB1 and/or CB2 receptor sites. Further, most of the analogs exhibit greater metabolic stability than arachidonylethanolamide. The improved receptor affinity and selectivity and/or greater metabolic stability make these analogs therapeutically useful as medications in individuals and animals for treatment of pain, glaucoma, epilepsy, nausea associated with chemotherapy, as well as suppression of the immune system, enhancement of appetite and in treatment of certain mental disorders.

    Abstract translation: 提出了对大麻素CB1和/或CB2受体位点具有高亲和力的新型复方壬酰胺。 此外,大多数类似物表现出比花生四烯酰乙酰胺更高的代谢稳定性。 改善的受体亲和力和选择性和/或更高的代谢稳定性使得这些类似物在个体和动物中用作治疗疼痛,青光眼,癫痫,与化学疗法相关的恶心以及抑制免疫系统,增加食欲和 治疗某些精神障碍。

    Method for the continuous production of tetra-substituted ureas
    5.
    发明授权
    Method for the continuous production of tetra-substituted ureas 失效
    连续生产四取代脲的方法

    公开(公告)号:US07053244B2

    公开(公告)日:2006-05-30

    申请号:US10520402

    申请日:2003-07-03

    CPC classification number: C07C273/1809 C07C275/06

    Abstract: The invention relates to a process for the preparation of tetrasubstituted ureas by reaction of the corresponding amines with phosgene in the presence of an aqueous inorganic base at a temperature in the range from 0 to 150° C., which comprises: feeding the corresponding amine, the phosgene and the aqueous inorganic base on average continuously to the reaction apparatus, forming a two-phase system in the reaction apparatus through the choice of the tetrasubstituted ureas to be prepared, through the mixing ratios of the substances and substance mixtures to be fed in, through the temperature during the reaction and, where appropriate, through the feed of an organic solvent which is not completely miscible with water, and discharging the reaction mixture on average continuously from the reaction apparatus.

    Abstract translation: 本发明涉及通过在无机碱水溶液存在下,在0至150℃的温度范围内使相应的胺与光气反应来制备四取代的脲的方法,该方法包括:将相应的胺, 光气和水无机碱平均连续向反应装置中,通过选择要制备的四取代脲形成反应装置中的两相体系,通过待进料的物质和物质混合物的混合比例 通过反应期间的温度,并且在适当的情况下,通过进料与水不完全混溶的有机溶剂,并从反应装置中连续排出反应混合物。

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