利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

20 条记录 (耗时 0.044 秒)

    MACROCYCLIC ANTAGONISTS OF THE MOTILIN RECEPTOR FOR TREATMENT OF GASTROINTESTINAL DYSMOTILITY DISORDERS
    5.
    发明申请
    MACROCYCLIC ANTAGONISTS OF THE MOTILIN RECEPTOR FOR TREATMENT OF GASTROINTESTINAL DYSMOTILITY DISORDERS 有权
    用于治疗胃肠疾病的动物感受因子的大分子拮抗剂

    公开(公告)号：US20100093720A1

    公开(公告)日：2010-04-15

    申请号：US12440802

    申请日：2007-09-11

    申请人： Eric Marsault ,  Graeme L. Fraser ,  Kamel Benakli ,  Carl St-Louis ,  Alain Rouillard ,  Helmut Thomas

    发明人： Eric Marsault ,  Graeme L. Fraser ,  Kamel Benakli ,  Carl St-Louis ,  Alain Rouillard ,  Helmut Thomas

    IPC分类号： A61K31/5377 ,  C07D487/00 ,  A61K31/33 ,  A61P1/00

    CPC分类号： C07K5/0812 ,  A61K38/00 ,  C07C271/16 ,  C07D273/00 ,  C07D413/06 ,  C07D417/12 ,  Y02P20/582

    摘要： The present invention provides conformationally-defined macrocyclic compounds that bind to and/or are functional modulators of the motilin receptor including subtypes, isoforms and/or variants thereof. These macrocyclic compounds, at a minimum, possess adequate pharmacological properties to be useful as therapeutics for a range of disease indications. In particular, these compounds are useful for treatment and prevention of disorders characterized by hypermotilinemia and/or gastrointestinal hypermotility, including, but not limited to, diarrhea, cancer treatment-related diarrhea, cancer-induced diarrhea, chemotherapy-induced diarrhea, radiation enteritis, radiation-induced diarrhea, stress-induced diarrhea, chronic diarrhea, AIDS-related diarrhea, C. difficile associated diarrhea, traveller's diarrhea, diarrhea induced by graph versus host disease, other types of diarrhea, dyspepsia, irritable bowel syndrome, chemotherapy-induced nausea and vomiting (emesis) and post-operative nausea and vomiting and functional gastrointestinal disorders. In addition, the compounds possess utility for the treatment of diseases and disorders characterized by poor stomach or intestinal absorption, such as short bowel syndrome, celiac disease and cachexia. The compounds also have use for the treatment of inflammatory diseases and disorders of the gastrointestinal tract, such as inflammatory bowel disease, ulcerative colitis, Crohn's disease and pancreatitis. Accordingly, methods of treating such disorders and pharmaceutical compositions including compounds of the present invention are also provided.

    摘要翻译： 本发明提供了构象定义的大环化合物，其与胃动素受体结合和/或是功能性调节剂，包括亚型，同种型和/或其变体。 这些大环化合物至少具有足够的药理学性质，可用作一系列疾病适应症的治疗剂。 特别地，这些化合物可用于治疗和预防以高肌钙蛋白血症和/或胃肠动力学特征为特征的疾病，包括但不限于腹泻，癌症治疗相关性腹泻，癌症引起的腹泻，化学疗法诱发的腹泻，放射性肠炎， 辐射诱发的腹泻，应激性腹泻，慢性腹泻，艾滋病相关性腹泻，艰难梭菌相关性腹泻，旅行者腹泻，图形与宿主病引起的腹泻，其他类型的腹泻，消化不良，肠易激综合征，化疗诱发的恶心 和呕吐（呕吐）和术后恶心呕吐和功能性胃肠道疾病。 此外，这些化合物具有治疗以肠胃吸收不良为特征的疾病和病症的用途，例如短肠综合症，乳糜泻和恶病质。 所述化合物还可用于治疗炎性疾病和胃肠道疾病，例如炎性肠病，溃疡性结肠炎，克罗恩病和胰腺炎。 因此，还提供了治疗这些病症的方法和包括本发明化合物的药物组合物。

    Macrocyclic antagonists of the motilin receptor for treatment of gastrointestinal dysmotility disorders
    6.
    发明授权
    Macrocyclic antagonists of the motilin receptor for treatment of gastrointestinal dysmotility disorders 有权
    胃动素障碍的胃动素受体大环拮抗剂

    公开(公告)号：US09133235B2

    公开(公告)日：2015-09-15

    申请号：US12440802

    申请日：2007-09-11

    申请人： Eric Marsault ,  Graeme L. Fraser ,  Kamel Benakli ,  Carl St-Louis ,  Alain Rouillard ,  Helmut Thomas

    发明人： Eric Marsault ,  Graeme L. Fraser ,  Kamel Benakli ,  Carl St-Louis ,  Alain Rouillard ,  Helmut Thomas

    IPC分类号： C07K5/087 ,  C07C271/16 ,  C07D273/00 ,  C07D413/06 ,  C07D417/12 ,  A61K38/00

    CPC分类号： C07K5/0812 ,  A61K38/00 ,  C07C271/16 ,  C07D273/00 ,  C07D413/06 ,  C07D417/12 ,  Y02P20/582

    摘要： The present invention provides conformationally-defined macrocyclic compounds that bind to and/or are functional modulators of the motilin receptor including subtypes, isoforms and/or variants thereof. These macrocyclic compounds, at a minimum, possess adequate pharmacological properties to be useful as therapeutics for a range of disease indications. In particular, these compounds are useful for treatment and prevention of disorders characterized by hypermotilinemia and/or gastrointestinal hypermotility, including, but not limited to, diarrhea, cancer treatment-related diarrhea, cancer-induced diarrhea, chemotherapy-induced diarrhea, radiation enteritis, radiation-induced diarrhea, stress-induced diarrhea, chronic diarrhea, AIDS-related diarrhea, C. difficile associated diarrhea, traveller's diarrhea, diarrhea induced by graph versus host disease, other types of diarrhea, dyspepsia, irritable bowel syndrome, chemotherapy-induced nausea and vomiting (emesis) and post-operative nausea and vomiting and functional gastrointestinal disorders. In addition, the compounds possess utility for the treatment of diseases and disorders characterized by poor stomach or intestinal absorption, such as short bowel syndrome, celiac disease and cachexia. The compounds also have use for the treatment of inflammatory diseases and disorders of the gastrointestinal tract, such as inflammatory bowel disease, ulcerative colitis, Crohn's disease and pancreatitis. Accordingly, methods of treating such disorders and pharmaceutical compositions including compounds of the present invention are also provided.

    摘要翻译： 本发明提供了构象定义的大环化合物，其与胃动素受体结合和/或是功能性调节剂，包括亚型，同种型和/或其变体。 这些大环化合物至少具有足够的药理学性质，可用作一系列疾病适应症的治疗剂。 特别地，这些化合物可用于治疗和预防以高肌钙蛋白血症和/或胃肠动力学特征为特征的疾病，包括但不限于腹泻，癌症治疗相关性腹泻，癌症引起的腹泻，化学疗法诱发的腹泻，放射性肠炎， 辐射诱发的腹泻，应激性腹泻，慢性腹泻，艾滋病相关性腹泻，艰难梭菌相关性腹泻，旅行者腹泻，图形与宿主病引起的腹泻，其他类型的腹泻，消化不良，肠易激综合征，化疗诱发的恶心 和呕吐（呕吐）和术后恶心呕吐和功能性胃肠道疾病。 此外，这些化合物具有治疗以肠胃吸收不良为特征的疾病和病症的用途，例如短肠综合症，乳糜泻和恶病质。 所述化合物还可用于治疗炎性疾病和胃肠道疾病，例如炎性肠病，溃疡性结肠炎，克罗恩病和胰腺炎。 因此，还提供了治疗这些病症的方法和包括本发明化合物的药物组合物。

    Macrocyclic modulators of the ghrelin receptor
    7.
    再颁专利
    Macrocyclic modulators of the ghrelin receptor 有权
    生长素释放肽受体的大环调节剂

    公开(公告)号：USRE42013E1

    公开(公告)日：2010-12-28

    申请号：US12636048

    申请日：2009-12-11

    申请人： Hamid Hoveyda ,  Mark L. Peterson ,  Graeme L. Fraser ,  Mahesh Ramaseshan

    发明人： Hamid Hoveyda ,  Mark L. Peterson ,  Graeme L. Fraser ,  Mahesh Ramaseshan

    IPC分类号： A61K38/12 ,  C07K5/12 ,  C07K1/00

    CPC分类号： C07K5/0808 ,  A61K38/00 ,  C07K5/0812

    摘要： The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.

    摘要翻译： 本发明提供已被证明是生长素释放肽受体（生长激素促分泌素受体，GHS-R1a和亚型，同种型及其变体）的选择性调节剂的新型构象定义的大环化合物。 本文还描述了合成新化合物的方法。 这些化合物可用作生长素释放肽受体的激动剂，并且用作治疗和预防一系列医学病症的药物，包括但不限于代谢和/或内分泌疾病，胃肠道疾病，心血管疾病，肥胖症和肥胖相关疾病， 中枢神经系统疾病，遗传疾病，过度增殖性疾病和炎症性疾病。

    MACROCYCLIC ANTAGONISTS OF THE MOTILIN RECEPTOR FOR MODULATION OF THE MIGRATING MOTOR COMPLEX
    10.
    发明申请
    MACROCYCLIC ANTAGONISTS OF THE MOTILIN RECEPTOR FOR MODULATION OF THE MIGRATING MOTOR COMPLEX 审中-公开
    用于调制电机复合材料的电磁感应器的大尺度拮抗剂

    公开(公告)号：US20080287371A1

    公开(公告)日：2008-11-20

    申请号：US12122094

    申请日：2008-05-16

    申请人： Graeme L. Fraser ,  Eric Marsault

    发明人： Graeme L. Fraser ,  Eric Marsault

    IPC分类号： A61K38/06 ,  A61P1/12

    CPC分类号： C07K5/0812 ,  A61K38/00 ,  C07K5/0821

    摘要： The present invention relates to novel conformationally-defined macrocyclic compounds that bind to and/or are functional modulators of the motilin receptor including subtypes, isoforms and/or variants thereof. These macrocyclic compounds are useful as therapeutics for a range of gastrointestinal disorders, in particular those in which suppression or inhibition of the migrating motor complex (MMC) is effective or malfunction of gastric motility or increased motilin secretion is observed, such as hypermotilinemia, imitable bowel syndrome, dyspepsia, including gallbladder dyspepsia, diarrhea, cancer treatment-related diarrhea, cancer-induced diarrhea, chemotherapy-induced diarrhea, radiation enteritis, radiation-induced diarrhea, stress-induced diarrhea, chronic diarrhea, AIDS-related diarrhea, C. difficile associated diarrhea, traveller's diarrhea, acute infectious diarrhea, diarrhea induced by graph versus host disease, other types of diarrhea, functional gastrointestinal disorders, chemotherapy-induced nausea and vomiting (emesis), post-operative nausea and vomiting, cyclic vomiting syndrome and functional vomiting. Accordingly, methods of treating such disorders with such macrocyclic compounds and pharmaceutical compositions thereof are also provided in addition to methods of modulating the migrating motor complex.

    摘要翻译： 本发明涉及与胃动素受体结合和/或功能调节剂的新型构象定义的大环化合物，包括亚型，同种型和/或其变体。 这些大环化合物可用作一系列胃肠道疾病的治疗剂，特别是那些抑制或抑制迁移性运动复合物（MMC）有效或者胃动力或增加的胃动素分泌异常的治疗剂，例如高肌钙蛋白血症，肠易激综合症 综合征，消化不良，包括胆囊消化不良，腹泻，癌症治疗相关性腹泻，癌症引起的腹泻，化疗引起的腹泻，放射性肠炎，放射性腹泻，应激性腹泻，慢性腹泻，艾滋病相关性腹泻，艰难梭菌 相关性腹泻，旅行者腹泻，急性感染性腹泻，图表与宿主病引起的腹泻，其他类型的腹泻，功能性胃肠道疾病，化疗诱发的恶心和呕吐（呕吐），术后恶心呕吐，呕吐综合征和功能性呕吐 。 因此，除了调节迁移运动复合物的方法之外，还提供了用这种大环化合物治疗这种病症的方法及其药物组合物。