UREA AND AMIDE DERIVATIVES OF AMINOALKYLPIPERAZINES AND USE THEREOF
    3.
    发明公开
    UREA AND AMIDE DERIVATIVES OF AMINOALKYLPIPERAZINES AND USE THEREOF 审中-公开
    联合国艾滋病毒/艾滋病毒/艾滋病毒/艾滋病毒/艾滋病毒

    公开(公告)号:EP2906221A4

    公开(公告)日:2016-03-09

    申请号:EP13846057

    申请日:2013-10-11

    申请人: SOUTHERN RES INST

    摘要: Provided are compounds represented by the formula: with Y, Ri, and R2 being defined in the present disclosure; pharmaceutically acceptable salts thereof, deuterated forms thereof, isomers thereof, solvates thereof, and mixtures thereof. The compounds can be used for treating a patient suffering from a condition capable of treatment with a partial agonist or antagonist of the dopamine D2/D3 receptors and are especially useful for patients suffering from schizophrenia, depressions, neurodegenerative diseases such as Parkinson's, dyskinesias, substance abuse and relapse to substance abuse and addiction to substances such as cocaine, methamphetamine, nicotine and alcohol, glaucoma, cognitive disorders, restless leg syndrome, attention deficit hyperactivity disorders, hyperprolactinemia, autism, motor disturbances such as akathisia, rigor, dystonias as well as various disorders of the urinary tract and other neurologic disorders. Also provided are processes for the preparation of compounds of the present disclosure.

    摘要翻译: 本发明提供了由下式表示的化合物:其中Y,R 1和R 2定义于本公开内容中; 其药学上可接受的盐,其氘代形式,其异构体,溶剂合物,及其混合物。 该化合物可用于治疗患有能够用多巴胺D2 / D3受体的部分激动剂或拮抗剂治疗的病症的患者,并且特别适用于患有精神分裂症,抑郁症,神经变性疾病如帕金森病,运动障碍,物质 滥用和复发药物滥用和成瘾物质如可卡因,甲基苯丙胺,尼古丁和酒精,青光眼,认知障碍,不宁腿综合征,注意缺陷多动障碍,高催乳素血症,自闭症,运动障碍如静坐,严重,肌张力障碍以及 各种尿路疾病和其他神经系统疾病。 还提供了制备本发明化合物的方法。

    HETEROCYCLE-FUSED MORPHINANS, USE THEREOF AND PREPARATION THEREOF
    5.
    发明公开
    HETEROCYCLE-FUSED MORPHINANS, USE THEREOF AND PREPARATION THEREOF 审中-公开
    赫尔辛基多瑙河

    公开(公告)号:EP2844661A4

    公开(公告)日:2015-11-11

    申请号:EP13784443

    申请日:2013-05-02

    申请人: SOUTHERN RES INST

    摘要: Provided are compounds of the formula: R1; R2, R3; R4; A; X; Y and Z are defined in the present disclosure; pharmaceutically acceptable salts thereof, deuterium forms thereof, isomers thereof, and mixture thereof; and processes for their preparation. The compounds can be used for treating a patient suffering from a condition that is capable of treatment with an agonist and/or antagonist of the opioid receptors and are especially useful a patient suffering from pain, treating a patient in need of an immunosuppressant to prevent rejection in organ transplant and skin graft, in need of an anti-allergic agent, in need of an anti-inflammatory agent, in need of a brain cell protectant, for drug and/or alcohol abuse, to decrease gastric secretion, for diarrhea, for cardiovascular disease, for a respiratory disease, in need of a cough and/or respiratory depressant, for mental illness, for epileptic seizures and other neurologic disorders.

    摘要翻译: 提供下式的化合物:R1; R2,R3; R4; 一个; X; Y和Z在本公开中定义; 其药学上可接受的盐,其氘形式,其异构体及其混合物; 及其制备方法。 该化合物可用于治疗患有可用阿片样物质受体的激动剂和/或拮抗剂治疗的病症的患者,并且对患有疼痛的患者特别有用,治疗需要免疫抑制剂的患者以防止排斥 在器官移植和皮肤移植中,需要抗过敏剂,需要抗炎剂,需要脑细胞保护剂,用于药物和/或酒精滥用,以减少胃分泌,腹泻,腹泻 心血管疾病,呼吸道疾病,需要咳嗽和/或呼吸抑制剂,精神疾病,癫痫发作和其他神经系统疾病。