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    Imidazole derivatives for the treatment of gastrointestinal disorders
    1.
    发明授权
    Imidazole derivatives for the treatment of gastrointestinal disorders 失效
    咪唑衍生物用于治疗胃肠道疾病

    公开(公告)号：US07745474B2

    公开(公告)日：2010-06-29

    申请号：US12158167

    申请日：2006-12-21

    申请人： Udo Bauer ,  Wayne Brailsford ,  Linda Gustafsson ,  Tor Svensson ,  Maria Saxin

    发明人： Udo Bauer ,  Wayne Brailsford ,  Linda Gustafsson ,  Tor Svensson ,  Maria Saxin

    IPC分类号： A61K31/417 ,  A61K31/4174 ,  C07D233/64 ,  C07D233/88

    CPC分类号： C07D233/90 ,  C07D405/12

    摘要： The present invention relates to novel imidazole derivatives having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). The compounds are represented by the general formula (I) wherein R1, R2, R3 and Y are as defined in the description. For example, R1 may be phenyl, R2 may be dimethylamino, R3 may be alkoxy and Y may be a thioylamino- or methyl eneamino- linked substitutuent containing an aryl group.

    摘要翻译： 本发明涉及具有正变构GABA B受体（GBR）调节剂作用的新型咪唑衍生物，用于制备所述化合物的方法及其用途，任选与GABAB激动剂组合用于抑制短暂食管括约肌松弛， 用于治疗胃食管反流疾病，以及治疗功能性胃肠道疾病和肠易激综合征（IBS）。 化合物由通式（I）表示，其中R 1，R 2，R 3和Y如说明书中所定义。 例如，R 1可以是苯基，R 2可以是二甲基氨基，R 3可以是烷氧基，Y可以是含有芳基的硫代氨基 - 或甲基烯氨基连接的取代基。

    Heterocyclic Gaba-b Modulators
    3.
    发明申请
    Heterocyclic Gaba-b Modulators 审中-公开
    杂环Gaba-b调制器

    公开(公告)号：US20080312291A1

    公开(公告)日：2008-12-18

    申请号：US12158183

    申请日：2006-12-21

    申请人： Udo Bauer ,  Linda Gustafsson ,  Maria Saxin ,  Tor Svensson

    发明人： Udo Bauer ,  Linda Gustafsson ,  Maria Saxin ,  Tor Svensson

    IPC分类号： C07D277/38 ,  A61K31/4439 ,  C07D417/02 ,  A61K31/426 ,  A61K31/421 ,  A61P1/00 ,  A61K31/422 ,  A61K31/427 ,  C07D263/48 ,  C07D413/02

    CPC分类号： C07D277/56 ,  A61K31/421 ,  A61K31/422 ,  A61K31/426 ,  A61K31/427 ,  A61K45/06 ,  C07C255/29 ,  C07D263/48 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  A61K2300/00

    摘要： The present invention relates to novel thiazole and oxazole derivatives having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). The compounds are represented by the general formula (I) wherein X1 and X2 are selected from 0 and N or S and N and R1, R2 and Y are as defined in the description. For example, R1 may be alkyl, alkoxy, thioalkoxy or aryl, R2 may be alkoxy and Y may be a carbonylamino-linked substituent containing an aryl or heteroaryl group.

    摘要翻译： 本发明涉及具有正变构GABA B受体（GBR）调节剂作用的新型噻唑和恶唑衍生物，用于制备所述化合物的方法及其用途，任选地与GABAB激动剂组合用于抑制短暂食管下括约肌 放松，用于治疗胃食管反流疾病，以及治疗功能性胃肠道疾病和肠易激综合征（IBS）。 化合物由通式（I）表示，其中X1和X2选自0和N或S和N，并且R1，R2和Y如说明书中所定义。 例如，R 1可以是烷基，烷氧基，硫代烷氧基或芳基，R 2可以是烷氧基，Y可以是含有芳基或杂芳基的羰基氨基连接的取代基。

    Imidazoles as Gaba- B Receptor Modulators
    7.
    发明申请
    Imidazoles as Gaba- B Receptor Modulators 审中-公开
    咪唑类作为Gaba- B受体调节剂

    公开(公告)号：US20080312305A1

    公开(公告)日：2008-12-18

    申请号：US12158159

    申请日：2006-12-21

    申请人： Udo Bauer ,  Linda Gustafsson ,  Maria Saxin

    发明人： Udo Bauer ,  Linda Gustafsson ,  Maria Saxin

    IPC分类号： A61K31/4164 ,  A61P1/00 ,  C07D233/90 ,  A61K31/4178 ,  C07D405/12

    CPC分类号： C07D233/90 ,  C07D233/88 ,  C07D405/12

    摘要： The present invention relates to novel imidazole derivatives having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). The compounds are represented by the general formula (I) wherein R1, R2, R3 and R4 are as defined in the description. For example, R1 may be alkyl or arylalkyl, R2 may be alkyl, R3 may be alkoxy and R4 may be a substituent containing an aryl group.

    摘要翻译： 本发明涉及具有正变构GABA B受体（GBR）调节剂作用的新型咪唑衍生物，用于制备所述化合物的方法及其用途，任选与GABAB激动剂组合用于抑制短暂食管括约肌松弛， 用于治疗胃食管反流疾病，以及治疗功能性胃肠道疾病和肠易激综合征（IBS）。 所述化合物由通式（I）表示，其中R 1，R 2，R 3和R 4如说明书中所定义。 例如，R 1可以是烷基或芳烷基，R 2可以是烷基，R 3可以是烷氧基，R 4可以是含有芳基的取代基。