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    Macrocyclic antagonists of the motilin receptor for treatment of gastrointestinal dysmotility disorders
    5.
    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.
    发明申请
    Macrocyclic Modulators of the Ghrelin Receptor 审中-公开
    生长素释放肽受体的大环调节剂

    公开(公告)号：US20090198050A1

    公开(公告)日：2009-08-06

    申请号：US12263179

    申请日：2008-10-31

    申请人： Eric Marsault ,  Luc Ouellet ,  Carl St-Louis ,  Sylvie Beaubien ,  Kamel Benakli ,  Hamid R. Hoveyda ,  Mark L. Peterson ,  Shridhar Bhat

    发明人： Eric Marsault ,  Luc Ouellet ,  Carl St-Louis ,  Sylvie Beaubien ,  Kamel Benakli ,  Hamid R. Hoveyda ,  Mark L. Peterson ,  Shridhar Bhat

    IPC分类号： C07D225/04 ,  C07D487/04 ,  C07C229/34 ,  C07D311/04

    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。

    Phenoxylpropanolamines, method for the production thereof and pharmaceutical compositions containing the same
    8.
    发明授权
    Phenoxylpropanolamines, method for the production thereof and pharmaceutical compositions containing the same 失效
    苯氧基丙醇胺，其制备方法和含有它们的药物组合物

    公开(公告)号：US06649627B1

    公开(公告)日：2003-11-18

    申请号：US09719640

    申请日：2001-03-26

    申请人： Roberto Cecchi ,  Tiziano Croci ,  Umberto Guzzi ,  Eric Marsault

    发明人： Roberto Cecchi ,  Tiziano Croci ,  Umberto Guzzi ,  Eric Marsault

    IPC分类号： A61K31445

    CPC分类号： C07D303/22 ,  C07D307/42 ,  C07D401/04 ,  C07D401/06 ,  C07D405/14

    摘要： The invention concerns compounds of formula (Ia) wherein R1a represents hydrogen, an —S(O)z —(C1-C4)Alk group, a —CO(C1-C4)Alk group, an —NHSO2—(C1-C4)Alk group, an NCHl (C1-C4) Alk group, a 2-furyl group or a halogen; R2 represents hydrogen or a (C1-C4)Alk group, a (C1-C4) alkoxyl group, a halogen, —COOH, —COO(C1-C4)Alk, —CN, —CONR3R4, —NO2, —SO2NH2, —NHSO2(C1-C4)Alk; m and n are independently 0, 1 or 2; R3 and R4 independently represent hydrogen or a (C1-C4)Alk group; Z is 1 or 2 and their salts or solvates, the pharmaceutical compositions that contain them, the process for their preparation, and intermediate synthesis products.

    摘要翻译： 本发明涉及式（Ia）化合物，其中R 1a表示氢，-S（O）z - （C 1 -C 4）Alk基，-CO（C 1 -C 4）Alk基，-NHSO 2 - （C 1 -C 4） 基团，NCH1（C1-C4）Alk基团，2-呋喃基或卤素; R2表示氢或（C1-C4）Alk基团，（C1-C4）烷氧基，卤素，-COOH， COO（C1-C4）Alk，-CN，-CONR3R4，-NO2，-SO2NH2，-NHSO2（C1-C4）Alk; m和n分别为0,1或2; R3和R4独立地表示氢或（C1 -C4）Alk基; Z为1或2及其盐或溶剂化物，含有它们的药物组合物，其制备方法和中间合成产物。

    Pharmaceutical salts of macrocyclic modulators of the ghrelin receptor
    10.
    发明授权
    Pharmaceutical salts of macrocyclic modulators of the ghrelin receptor 有权
    生长素释放肽受体的大环调节剂的药物盐

    公开(公告)号：US08334256B2

    公开(公告)日：2012-12-18

    申请号：US12351395

    申请日：2009-01-09

    申请人： Eric Marsault ,  Carl St-Louis

    发明人： Eric Marsault ,  Carl St-Louis

    IPC分类号： A61K38/25 ,  C09F1/04

    CPC分类号： C07K5/0827 ,  A61K38/00 ,  C07D273/00 ,  C07D498/08 ,  C07K5/0808 ,  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。