1,4-dithiin and 1,4-dithiepin-1,1,4,4, tetroxide derivatives useful as antagonists of the human galanin receptor
    41.
    发明授权
    1,4-dithiin and 1,4-dithiepin-1,1,4,4, tetroxide derivatives useful as antagonists of the human galanin receptor 有权
    可用作人甘丙肽受体拮抗剂的1,4-二硫辛酸和1,4-二硫辛啶-1,1,4,4四氧化物衍生物

    公开(公告)号:US06407136B1

    公开(公告)日:2002-06-18

    申请号:US09563147

    申请日:2000-05-02

    IPC分类号: A61K31385

    摘要: The invention is directed to 1,4-dithiin- and 1,4-dithiepin-1,1,4,4-tetroxide derivatives useful as galanin receptor antagonists for treating disorders of the central nervous system. Pharmaceutical compositions comprising the compounds of the present invention and methods of treating conditions such as an eating disorder, obesity, bulimia nervosa, anorexia nervosa, binge eating, diabetes, dyslipidemia, hypertension, memory loss, sleep disturbances, pain, depression, anxiety, Alzheimer's disease, senile dementia, cerebral hemorrhage, or diarrhea are also described.

    摘要翻译: 本发明涉及用作治疗中枢神经系统疾病的甘丙肽受体拮抗剂的1,4-二硫辛酸和1,4-二硫辛啶-1,1,4,4-四氧化物衍生物。 包含本发明化合物的药物组合物和治疗诸如进食障碍,肥胖症,神经性贪食症,神经性厌食症,暴饮暴食症,糖尿病,血脂异常,高血压,记忆丧失,睡眠障碍,疼痛,抑郁,焦虑,阿尔茨海默病 还描述了疾病,老年性痴呆,脑出血或腹泻。

    Process for production of 1,4-bis(difluoroalkyl)benzene derivative
    42.
    发明授权
    Process for production of 1,4-bis(difluoroalkyl)benzene derivative 失效
    生产1,4-双(二氟烷基)苯衍生物的方法

    公开(公告)号:US6384289B2

    公开(公告)日:2002-05-07

    申请号:US75860701

    申请日:2001-01-11

    摘要: A process is provided which allows a 1,4-bis(difluoroalkyl)benzene derivative to be produced inexpensively by a simple procedure without requiring any special facility. This process comprises causing a compound (A) of the following formula (1):wherein X1, X2, X3, and X4 independently stand for an oxygen or sulfur atom, Y1 and Y2 independently stand for a group of the formula: -CnH2n-, in which n is 2 or 3, k is an integer in the range of 0 to 4, G stands for a halogen group, an alkyl group, a perfluoroalkyl group, or an alkoxy group, and m is an integer in the range of 0 to 4, to react with a fluorine-containing species, the molar ratio of the fluorine-containing species to compound (A) being in the range of 20-40. The process is carried out in the presence of a bromine-containing compound, which is in an amount of 2 to 3 equivalences to the amount of compound (A), in an organic solvent at -80° C. to 30° C., the final concentration of compound (A) being in the range of 3 to 30% by weight.

    摘要翻译: 提供了一种方法,其允许通过简单的方法廉价地生产1,4-双(二氟烷基)苯衍生物,而不需要任何特殊设备。 该方法包括使下式(1)的化合物(A):其中X1,X2,X3和X4独立地代表氧或硫原子,Y1和Y2独立地表示下式的基团:-CnH2n- ,其中n为2或3,k为0至4的整数,G表示卤素基团,烷基,全氟烷基或烷氧基,m为在 0至4,与含氟物质反应时,含氟物质与化合物(A)的摩尔比在20-40范围内。 该方法在-80℃至30℃的有机溶剂中,在化合物(A)的量为2〜3当量的含溴化合物的存在下进行, 化合物(A)的最终浓度在3〜30重量%的范围内。