Guanidine derivatives and their use as neuropeptide ff receptor antagonists
    12.
    发明申请
    Guanidine derivatives and their use as neuropeptide ff receptor antagonists 失效
    胍衍生物及其作为神经肽ff受体拮抗剂的用途

    公开(公告)号:US20060194788A1

    公开(公告)日:2006-08-31

    申请号:US10549685

    申请日:2004-03-22

    摘要: The invention relates to guanidine derivatives of formula (I) where: A represents a chain of 3-6 carbon atoms, one of which can be replaced by —N(R′)— or —O— and R′ is H or a substituent; the ring skeleton only contains both double bonds of the thiazole component; the pharmaceutically-acceptable acid addition salts of basic compounds of formula (I), the pharmaceutically-acceptable salts of compounds of formula (I), comprising acid groups, with bases, the pharmaceutically-acceptable esters of hydroxy or carboxyl group containing compounds of formula (I) and the solvates or hydrates thereof, which exhibit a neuropeptide FF receptor antagonist effect. The above are suitable for the treatment of pain and hyperalgesia, withdrawal symptoms in alcohol, psychotropic and nicotine dependencies, for improvement or cure of said dependencies, for regulation of insulin excretion, food intake, memory functions, blood pressure, electrolyte and energy management and for treatment of urinary incontinence. The above can be produced using generally used methods and processed to give medicaments.

    摘要翻译: 本发明涉及式(I)的胍衍生物,其中:A表示3-6个碳原子的链,其中一个可以被-N(R') - 或-O-代替,R'是H或取代基 ; 环骨架仅含有噻唑组分的双键; 式(I)的碱性化合物的药学上可接受的酸加成盐,包含酸基的式(I)化合物与碱的药学上可接受的盐,含有羟基或羧基的式 (I)及其溶剂合物或水合物,其表现出神经肽FF受体拮抗剂作用。 以上适用于治疗疼痛和痛觉过敏,酒精戒断症状,​​精神药物和尼古丁依赖性,用于改善或治愈所述依赖性,调节胰岛素排泄,食物摄取,记忆功能,血压,电解质和能量管理以及 用于治疗尿失禁。 上述可以使用通常使用的方法制备并加工以得到药物。

    2,3,4,9-tetrahydro-1H-carbazole derivatives as CRTH2 receptor antagonists
    13.
    发明授权
    2,3,4,9-tetrahydro-1H-carbazole derivatives as CRTH2 receptor antagonists 有权
    2,3,4,9-四氢-1H-咔唑衍生物作为CRTH2受体拮抗剂

    公开(公告)号:US08039474B2

    公开(公告)日:2011-10-18

    申请号:US11722095

    申请日:2005-12-22

    CPC分类号: C07D209/88

    摘要: The invention relates to novel tetrahydro-1H-carbazole derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and methods of treatment comprising administration of said compounds to patients.

    摘要翻译: 本发明涉及新四氢-1H-咔唑衍生物及其在制备药物组合物中作为活性成分的用途。 本发明还涉及包括制备化合物的方法,含有一种或多种这些化合物的药物组合物和包括向患者施用所述化合物的治疗方法的相关方面。

    Pyrazolidinedione derivatives
    17.
    发明申请
    Pyrazolidinedione derivatives 审中-公开
    吡唑烷二酮衍生物

    公开(公告)号:US20070037846A1

    公开(公告)日:2007-02-15

    申请号:US10562623

    申请日:2004-06-16

    摘要: The present invention relates to compounds of alkylidene pyrazolidinedione derivatives, which are effective platelet ADP receptor antagonists that prevent platelet aggregation and thrombosis. Thus, the present invention also relates to pharmaceutical compositions that contain the compounds as well as methods of preventing or treating peripheral, visceral, hepatic, renal, cardio- and cerebro-vascular diseases and conditions that are associated with platelet aggregation, including thrombosis, in humans and other mammals. The present invention further provides a process for manufacturing the alkylidene pyrazolidinedione derivatives.

    摘要翻译: 本发明涉及亚烷基吡唑烷二酮衍生物的化合物,其是有效的血小板聚集和血栓形成的血小板ADP受体拮抗剂。 因此,本发明还涉及含有化合物的药物组合物以及预防或治疗外周,内脏,肝,肾,心脑血管疾病和与血小板聚集相关的病症的方法,包括血栓形成 人类和其他哺乳动物。 本发明还提供了制备亚烷基吡唑烷二酮衍生物的方法。

    (3-amino-1,2,3,4-tetrahydro-9 H-carbazol-9-yl)-acetic acid derivatives
    19.
    发明授权
    (3-amino-1,2,3,4-tetrahydro-9 H-carbazol-9-yl)-acetic acid derivatives 有权
    (3-氨基-1,2,3,4-四氢-9H-咔唑-9-基) - 乙酸衍生物

    公开(公告)号:US08143304B2

    公开(公告)日:2012-03-27

    申请号:US12376932

    申请日:2007-08-02

    CPC分类号: C07D209/88

    摘要: The present invention relates to (3-amino-1,2,3,4-tetrahydro-9H-carbazol-9-yl)-acetic acid derivatives of Formula (I) wherein R1, R2, R3, R4, R5 and R6 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.

    摘要翻译: 本发明涉及式(I)的(3-氨基-1,2,3,4-四氢-9H-咔唑-9-基) - 乙酸衍生物,其中R 1,R 2,R 3,R 4,R 5和R 6是 如在描述中所描述的,以及它们作为前列腺素受体调节剂的用途,最特别地作为前列腺素D2受体调节剂在治疗各种前列腺素介导的疾病和病症中的用途,含有这些化合物的药物组合物及其制备方法。