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    MACROCYCLIC ANTAGONISTS OF THE MOTILIN RECEPTOR FOR TREATMENT OF GASTROINTESTINAL DYSMOTILITY DISORDERS
    1.
    发明公开
    MACROCYCLIC ANTAGONISTS OF THE MOTILIN RECEPTOR FOR TREATMENT OF GASTROINTESTINAL DYSMOTILITY DISORDERS 有权
    大环胃动素拮抗剂胃肠道疾病的治疗

    公开(公告)号：EP2054429A2

    公开(公告)日：2009-05-06

    申请号：EP07838009.4

    申请日：2007-09-11

    申请人： Tranzyme Pharma, Inc.

    发明人： MARSAULT, Éric ,  FRASER, Graeme ,  BENAKLI, Kamel ,  ST-LOUIS, Carl ,  ROUILLARD, Alain ,  THOMAS, Helmut

    IPC分类号： C07K5/08 ,  A61P1/00 ,  C07C271/16 ,  C07D213/64 ,  C07D213/65

    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.

    METHODS OF USING MACROCYCLIC INHIBITORS OF SERINE PROTEASE ENZYMES
    5.
    发明公开
    METHODS OF USING MACROCYCLIC INHIBITORS OF SERINE PROTEASE ENZYMES 审中-公开
    使用方法的丝氨酸蛋白酶的酶的MACRO循环抑制剂的

    公开(公告)号：EP2491020A1

    公开(公告)日：2012-08-29

    申请号：EP10825750.2

    申请日：2010-10-22

    申请人： Tranzyme Pharma, Inc. ,  Université de Sherbrooke

    发明人： MARSAULT, Éric ,  LEOGANE, Olivier ,  MATHIEU, Axel ,  BEAUBIEN, Sylvie ,  LEDUC, Richard

    IPC分类号： C07D225/00

    CPC分类号： A61K31/395

    摘要： The present invention relates to novel macrocyclic compounds and salts thereof that bind to and/or are inhibitors of serine protease enzymes and methods of using the compounds. The present invention also relates to intermediates of these compounds, pharmaceutical compositions containing these compounds and methods of using the same. These compounds are useful as therapeutics for treatment and prevention of a range of disease indications including hyperproliferative disorders, in particular those characterized by tumor metastasis, inflammatory disorders, skin and tissue disorders, cardiovascular disorders, respiratory disorders and viral infections.

    MACROCYCLIC INHIBITORS OF SERINE PROTEASE ENZYMES
    6.
    发明公开
    MACROCYCLIC INHIBITORS OF SERINE PROTEASE ENZYMES 审中-公开
    丝氨酸蛋白酶的酶的MACRO CYCLIC抑制剂

    公开(公告)号：EP2491004A2

    公开(公告)日：2012-08-29

    申请号：EP10825746.0

    申请日：2010-10-22

    申请人： Tranzyme Pharma, Inc.

    发明人： MARSAULT, Éric ,  LEOGANE, Olivier ,  MATHIEU, Axel ,  BEAUBIEN, Sylvie

    IPC分类号： C07C225/00

    CPC分类号： A61K31/395

    摘要： The present invention relates to novel macrocyclic compounds and salts thereof that bind to and/or are inhibitors of serine protease enzymes. The present invention also relates to intermediates of these compounds, pharmaceutical compositions containing these compounds and methods of using the compounds. These compounds are useful as therapeutics for treatment and prevention of a range of disease indications including hyperproliferative disorders, in particular those characterized by tumor metastasis, inflammatory disorders, skin and tissue disorders, cardiovascular disorders, respiratory disorders and viral infections.