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公开(公告)号：US07179807B2
公开(公告)日：2007-02-20
申请号：US10645312
申请日：2003-08-20
申请人： Taeyoung Yoon , Ping Ge , Stéphane De Lombaert , Raymond F. Horvath , Dario Doller , Kevin J. Hodgetts , Lu Yan Zhang , Bernd Kaiser , Xuechun Zhang , Yasuchika Yamaguchi , Cunyu Zhang , Jim Darrow
发明人： Taeyoung Yoon , Ping Ge , Stéphane De Lombaert , Raymond F. Horvath , Dario Doller , Kevin J. Hodgetts , Lu Yan Zhang , Bernd Kaiser , Xuechun Zhang , Yasuchika Yamaguchi , Cunyu Zhang , Jim Darrow
IPC分类号： A61K31/535 , A61K31/497 , A61K31/4965 , C07D413/00 , C07D403/00
CPC分类号： C07D241/12 , C07D241/18 , C07D241/20 , C07D241/26 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/04
摘要： Novel 5-substituted-2-arylpyrazine compounds are provided. Such compounds can act as selective modulators or CRF receptors. Compounds of the invention are provided by the following formula: The 5-substituted-2-arylpyrazine compounds provided herein are useful in the treatment of a number of CNS and periphercal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided.Compounds provided are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.
摘要翻译： 提供新的5-取代-2-芳基吡嗪化合物。 这些化合物可以作为选择性调节剂或CRF受体。 本发明化合物由下式提供：本文提供的5-取代-2-芳基吡嗪化合物可用于治疗多种CNS和外周疾病，特别是压力，焦虑，抑郁，心血管疾病和进食障碍。 还提供了治疗这种疾病以及包装的药物组合物的方法。 提供的化合物也可用作CRF受体定位的探针，并且作为用于CRF受体结合的测定中的标准物。 给出了在受体定位研究中使用化合物的方法。
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公开(公告)号：US07202250B2
公开(公告)日：2007-04-10
申请号：US11107148
申请日：2005-04-15
申请人： Taeyoung Yoon , Ping Ge , Raymond F. Horvath , Stėphane DeLombaert , Kevin J. Hodgetts , Dario Doller , Cunyu Zhang
发明人： Taeyoung Yoon , Ping Ge , Raymond F. Horvath , Stėphane DeLombaert , Kevin J. Hodgetts , Dario Doller , Cunyu Zhang
IPC分类号： A61K31/4965 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00
CPC分类号： C07D401/04 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/5355 , C07D241/12 , C07D241/18 , C07D241/20 , C07D401/12 , C07D403/04 , C07D405/12 , C07D409/04
摘要： Arylpyrazine compounds are provided, including arylpyrazines that can bind with high affinity and high selectivity to CRF1 receptors, including human CRF1 receptors. The invention thus includes methods for treatment of disorders and diseases associated with CRF1 receptors, including CNS-related disorders and diseases, particularly affective disorders and diseases, and acute and chronic neurological disorders and diseases.
摘要翻译： 提供了芳基吡嗪化合物，包括可以以高亲和力和对CRF 1受体（包括人CRF 1受体）的高选择性结合的芳基吡嗪。 因此，本发明包括治疗与CRF 1受体相关的疾病和疾病的方法，包括CNS相关疾病和疾病，特别是情感障碍和疾病，以及急性和慢性神经障碍和疾病。
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公开(公告)号：US20070043056A1
公开(公告)日：2007-02-22
申请号：US11585405
申请日：2006-10-23
申请人： Taeyoung Yoon , Ping Ge , Stephane De Lombaert , Raymond Horvath , Dario Doller , Kevin Hodgetts , Lu Yan Zhang , Bernd Kaiser , Xuechun Zhang , Cunyu Zhang , Jim Darrow , Yasuchika Yamaguchi
发明人： Taeyoung Yoon , Ping Ge , Stephane De Lombaert , Raymond Horvath , Dario Doller , Kevin Hodgetts , Lu Yan Zhang , Bernd Kaiser , Xuechun Zhang , Cunyu Zhang , Jim Darrow , Yasuchika Yamaguchi
IPC分类号： A61K31/4965 , A61K31/497 , C07D403/04
CPC分类号： C07D241/12 , C07D241/18 , C07D241/20 , C07D241/26 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/04
摘要： Novel 5-substituted-2-arylpyrazine compounds are provided. Such compounds can act as selective modulators of CRF receptors. The 5-substituted-2-arylpyrazine compounds provided herein are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds provided are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.
摘要翻译： 提供新的5-取代-2-芳基吡嗪化合物。 这些化合物可以作为CRF受体的选择性调节剂。 本文提供的5-取代-2-芳基吡嗪化合物可用于治疗许多CNS和周围疾病，特别是压力，焦虑，抑郁，心血管疾病和进食障碍。 还提供了治疗这种疾病以及包装的药物组合物的方法。 提供的化合物也可用作CRF受体定位的探针，并且作为用于CRF受体结合的测定中的标准物。 给出了在受体定位研究中使用化合物的方法。
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4.发明申请公开(公告)号：US20100222345A1
公开(公告)日：2010-09-02
申请号：US12376577
申请日：2007-08-08
申请人： Caroline Jean Diaz , Curt Dale Haffner , Jason Daniel Speake , Cunyu Zhang , Wendy Yoon Mills , Paul Kenneth Spearing , David John Cowan , Gary Martin Green
发明人： Caroline Jean Diaz , Curt Dale Haffner , Jason Daniel Speake , Cunyu Zhang , Wendy Yoon Mills , Paul Kenneth Spearing , David John Cowan , Gary Martin Green
IPC分类号： A61K31/4184 , C07D235/04 , C07D413/12 , C07D405/12 , C07D471/04 , C07D401/10 , A61K31/5377 , A61K31/4439 , A61K31/4725
CPC分类号： C07D235/08 , C07D209/08 , C07D231/56 , C07D263/56 , C07D401/04 , C07D417/04 , C07D471/04 , C07D487/04
摘要： This invention relates to novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy.
摘要翻译： 本发明涉及作为一种或多种阿片受体的拮抗剂或反向激动剂的新化合物，含有它们的药物组合物，其制备方法及其在治疗中的用途。
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公开(公告)号：US20070225287A1
公开(公告)日：2007-09-27
申请号：US11675648
申请日：2007-02-16
申请人： Taeyoung Yoon , Ping Ge , Raymond Horvath , Stephane DeLombaert , Kevin Hodgetts , Dario Doller , Cunyu Zhang
发明人： Taeyoung Yoon , Ping Ge , Raymond Horvath , Stephane DeLombaert , Kevin Hodgetts , Dario Doller , Cunyu Zhang
IPC分类号： A61K31/4965 , A61K31/496 , A61K31/497 , A61K31/5355
CPC分类号： C07D401/04 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/5355 , C07D241/12 , C07D241/18 , C07D241/20 , C07D401/12 , C07D403/04 , C07D405/12 , C07D409/04
摘要： Arylpyrazine compounds are provided, including arylpyrazines that can bind with high affinity and high selectivity to CRF1 receptors, including human CRF1 receptors. The invention thus includes methods for treatment of disorders and diseases associated with CRF1 receptors, including CNS-related disorders and diseases, particularly affective disorders and diseases, and acute and chronic neurological disorders and diseases.
摘要翻译： 提供了芳基吡嗪化合物，包括可以以高亲和力和对CRF 1受体（包括人CRF 1受体）的高选择性结合的芳基吡嗪。 因此，本发明包括治疗与CRF 1受体相关的疾病和疾病的方法，包括CNS相关疾病和疾病，特别是情感障碍和疾病，以及急性和慢性神经障碍和疾病。
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公开(公告)号：US06995161B2
公开(公告)日：2006-02-07
申请号：US09788315
申请日：2001-02-16
申请人： Taeyoung Yoon , Ping Ge , Raymond F. Horvath , Stephane DeLombaert , Kevin J. Hodgetts , Dario Doller , Cunyu Zhang
发明人： Taeyoung Yoon , Ping Ge , Raymond F. Horvath , Stephane DeLombaert , Kevin J. Hodgetts , Dario Doller , Cunyu Zhang
IPC分类号： A61K31/4965 , C07D241/20
CPC分类号： C07D401/04 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/5355 , C07D241/12 , C07D241/18 , C07D241/20 , C07D401/12 , C07D403/04 , C07D405/12 , C07D409/04
摘要： Arylpyrazine compounds are provided, including arylpyrazines that can bind with high affinity and high selectivity to CRF1 receptors, including human CRF1 receptors. The invention thus includes methods for treatment of disorders and diseases associated with CRF1 receptors, including CNS-related disorders and diseases, particularly affective disorders and diseases, and acute and chronic neurological disorders and diseases.
摘要翻译： 提供了芳基吡嗪化合物，包括可以以高亲和力和对CRF 1受体（包括人CRF 1受体）的高选择性结合的芳基吡嗪。 因此，本发明包括治疗与CRF 1受体相关的疾病和疾病的方法，包括CNS相关疾病和疾病，特别是情感障碍和疾病，以及急性和慢性神经障碍和疾病。
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公开(公告)号：US08633175B2
公开(公告)日：2014-01-21
申请号：US12376580
申请日：2007-08-08
申请人： David John Cowan , Andrew Lamont Larkin , Cunyu Zhang , David Lee Musso , Gary Martin Green , Rodolfo Cadilla , Paul Kenneth Spearing , Michael Joseph Bishop , Jason Daniel Speake
发明人： David John Cowan , Andrew Lamont Larkin , Cunyu Zhang , David Lee Musso , Gary Martin Green , Rodolfo Cadilla , Paul Kenneth Spearing , Michael Joseph Bishop , Jason Daniel Speake
CPC分类号： C07C237/48 , A61K31/166 , A61K31/381 , A61K31/4406 , A61K31/4468 , A61K31/472 , A61K31/495 , A61K31/5375 , A61K45/06 , C07C53/18 , C07C233/25 , C07C235/42 , C07C237/30 , C07C311/08 , C07C323/25 , C07C2601/14 , C07C2601/18 , C07C2602/08 , C07C2602/42 , C07C2603/74 , C07D209/08 , C07D211/60 , C07D213/38 , C07D213/56 , C07D213/81 , C07D217/02 , C07D217/04 , C07D231/12 , C07D233/64 , C07D233/70 , C07D233/72 , C07D249/06 , C07D249/08 , C07D249/10 , C07D271/06 , C07D275/02 , C07D277/32 , C07D285/10 , C07D307/52 , C07D333/20 , C07D333/24 , C07D333/38 , C07D401/10 , C07D417/12
摘要： Novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, pharmaceutical compositions containing them, to processes for their preparation.
摘要翻译： 作为一种或多种阿片受体的拮抗剂或反向激动剂的新型化合物，含有它们的药物组合物，其制备方法。
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8.发明申请公开(公告)号：US20110124559A1
公开(公告)日：2011-05-26
申请号：US12376580
申请日：2007-08-08
申请人： David John Cowan , Andrew Lamont Larkin , Cunyu Zhang , David Lee Musso , Gary Martin Green , Rodolfo Cadilla , Paul Kenneth Spearing , Michael Joseph Bishop , Jason Daniel Speake
发明人： David John Cowan , Andrew Lamont Larkin , Cunyu Zhang , David Lee Musso , Gary Martin Green , Rodolfo Cadilla , Paul Kenneth Spearing , Michael Joseph Bishop , Jason Daniel Speake
IPC分类号： A61K38/18 , C07D249/08 , A61K38/22 , A61K31/4196 , A61P3/04 , A61P3/10 , A61P9/12 , A61P25/24 , A61P25/22 , A61P25/30
CPC分类号： C07C237/48 , A61K31/166 , A61K31/381 , A61K31/4406 , A61K31/4468 , A61K31/472 , A61K31/495 , A61K31/5375 , A61K45/06 , C07C53/18 , C07C233/25 , C07C235/42 , C07C237/30 , C07C311/08 , C07C323/25 , C07C2601/14 , C07C2601/18 , C07C2602/08 , C07C2602/42 , C07C2603/74 , C07D209/08 , C07D211/60 , C07D213/38 , C07D213/56 , C07D213/81 , C07D217/02 , C07D217/04 , C07D231/12 , C07D233/64 , C07D233/70 , C07D233/72 , C07D249/06 , C07D249/08 , C07D249/10 , C07D271/06 , C07D275/02 , C07D277/32 , C07D285/10 , C07D307/52 , C07D333/20 , C07D333/24 , C07D333/38 , C07D401/10 , C07D417/12
摘要： Novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, pharmaceutical compositions containing them, to processes for their preparation.
摘要翻译： 作为一种或多种阿片受体的拮抗剂或反向激动剂的新型化合物，含有它们的药物组合物，其制备方法。
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公开(公告)号：US20050215559A1
公开(公告)日：2005-09-29
申请号：US11107148
申请日：2005-04-15
申请人： Taeyoung Yoon , Ping Ge , Raymond Horvath , Stephane DeLombaert , Kevin Hodgetts , Dario Doller , Cunyu Zhang
发明人： Taeyoung Yoon , Ping Ge , Raymond Horvath , Stephane DeLombaert , Kevin Hodgetts , Dario Doller , Cunyu Zhang
IPC分类号： A61K31/4965 , A61K31/5377 , A61P1/00 , A61P1/04 , A61P9/10 , A61P9/12 , A61P15/00 , A61P19/10 , A61P25/00 , A61P25/18 , A61P25/22 , A61P25/24 , A61P43/00 , C07D241/00 , C07D241/12 , C07D241/18 , C07D241/20 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/04 , C07D239/02
CPC分类号： C07D401/04 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/5355 , C07D241/12 , C07D241/18 , C07D241/20 , C07D401/12 , C07D403/04 , C07D405/12 , C07D409/04
摘要： Arylpyrazine compounds are provided, including arylpyrazines that can bind with high affinity and high selectivity to CRF1 receptors, including human CRF1 receptors. The invention thus includes methods for treatment of disorders and diseases associated with CRF1 receptors, including CNS-related disorders and diseases, particularly affective disorders and diseases, and acute and chronic neurological disorders and diseases.
摘要翻译： 提供了芳基吡嗪化合物，包括可以以高亲和力和对CRF 1受体（包括人CRF 1受体）的高选择性结合的芳基吡嗪。 因此，本发明包括治疗与CRF 1受体相关的疾病和疾病的方法，包括CNS相关疾病和疾病，特别是情感障碍和疾病，以及急性和慢性神经障碍和疾病。
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