-
公开(公告)号:US20050234051A1
公开(公告)日:2005-10-20
申请号:US11147895
申请日:2005-06-07
申请人: Kevin Hodgetts , Dario Doller
发明人: Kevin Hodgetts , Dario Doller
IPC分类号: G01N33/50 , A61J1/14 , A61K31/513 , A61K31/5377 , A61K31/541 , A61K31/55 , A61P1/04 , A61P1/12 , A61P1/14 , A61P3/04 , A61P5/14 , A61P9/04 , A61P9/12 , A61P15/08 , A61P17/06 , A61P19/02 , A61P25/18 , A61P25/22 , A61P25/24 , A61P29/00 , A61P37/08 , A61P43/00 , C07D239/34 , C07D239/36 , C07D239/46 , C07D239/47 , C07D239/52 , C12Q1/02 , G01N33/15 , G01N33/58 , C07D413/02 , C07D417/02 , C07D43/02
CPC分类号: C07D239/36 , C07D239/47 , C07D239/52
摘要: Arylpyrimidinone compounds that act as selective modulators of CRF 1 receptors are provided. These compounds 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 of the invention 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: 提供作为CRF 1受体的选择性调节剂的芳基嘧啶酮化合物。 这些化合物可用于治疗许多中枢神经系统和周围疾病,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。 本发明的化合物也可用作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。
-
公开(公告)号:US20060009456A1
公开(公告)日:2006-01-12
申请号:US11154986
申请日:2005-06-16
申请人: Alan Hutchinson , Bertrand Chenard , Guiying Li , Manuka Ghosh , James Tarrant , Taeyoung Yoon , George Luke , Kyungae Lee , Mary-Margaret O'Donnell , Wallace Pringle , John Peterson , Kevin Hodgetts , Cheryl Steenstra , Dario Doller
发明人: Alan Hutchinson , Bertrand Chenard , Guiying Li , Manuka Ghosh , James Tarrant , Taeyoung Yoon , George Luke , Kyungae Lee , Mary-Margaret O'Donnell , Wallace Pringle , John Peterson , Kevin Hodgetts , Cheryl Steenstra , Dario Doller
IPC分类号: A61K31/498 , A61K31/497 , A61K31/496 , C07D403/02 , C07D487/04
CPC分类号: C07D295/073 , C07D207/08 , C07D207/12 , C07D207/26 , C07D207/38 , C07D211/18 , C07D211/34 , C07D211/38 , C07D211/42 , C07D211/46 , C07D211/52 , C07D211/74 , C07D213/64 , C07D213/74 , C07D213/82 , C07D231/12 , C07D233/54 , C07D233/56 , C07D249/04 , C07D249/08 , C07D257/04 , C07D261/08 , C07D275/02 , C07D295/088 , C07D295/096 , C07D295/192 , C07D307/20 , C07D307/79 , C07D307/82 , C07D309/06 , C07D309/12 , C07D311/14 , C07D401/12 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/08
摘要: Aryl-substituted piperazine derivatives are provided. Such compounds may be used to modulate MCH receptor activity in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).
摘要翻译: 提供了芳基取代的哌嗪衍生物。 这样的化合物可用于在体内或体外调节MCH受体活性,并且特别可用于治疗人,驯养伴侣动物和家畜中的各种代谢,喂养和性障碍。 还提供了用于治疗这种病症的药物组合物和方法,以及使用这些配体检测MCH受体的方法(例如受体定位研究)。
-
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。
-
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。
-
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。
-
公开(公告)号:US20070043049A1
公开(公告)日:2007-02-22
申请号:US10564431
申请日:2004-07-09
申请人: Rajagopal Bakthavatchalam , Kevin Hodgetts , Alan Hutchison , Robert Ohliger , Taeyoung Yoon , Xiaozhang Zheng
发明人: Rajagopal Bakthavatchalam , Kevin Hodgetts , Alan Hutchison , Robert Ohliger , Taeyoung Yoon , Xiaozhang Zheng
IPC分类号: A61K31/53
CPC分类号: C07D401/12 , A61K31/506 , A61K31/53 , C07D251/52 , C07D251/54 , C07D401/14 , G01N33/566
摘要: Substituted heterocyclic diarylamine analogues of Formula I are provided: wherein X, Y and Z are independently N or optionally substituted C, and other variables are as described in the specification. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译: 提供式I的取代的杂环二芳基胺类似物:其中X,Y和Z独立地为N或任选被取代的C,并且其它变量如说明书中所述。 这些化合物是可用于在体内或体外调节特异性受体活性的配体,并且特别可用于治疗与人类,驯养伴侣动物和家畜中的病理受体激活相关的病症。 还提供了用于治疗这些病症的药物组合物和方法,以及使用这些配体进行受体定位研究的方法。
-
公开(公告)号:US20060111337A1
公开(公告)日:2006-05-25
申请号:US11250135
申请日:2005-10-12
申请人: Rajagopal Bakthavatchalam , Timothy Caldwell , Bertrand Chenard , Kevin Hodgetts , Scott Capitosti
发明人: Rajagopal Bakthavatchalam , Timothy Caldwell , Bertrand Chenard , Kevin Hodgetts , Scott Capitosti
IPC分类号: A61K31/506 , A61K31/5377 , A61K31/501 , A61K31/498 , A61K31/497 , A61K31/496 , A61K31/4745 , C07D471/02 , C07D487/02
CPC分类号: C07D471/04 , C07D401/04 , C07D401/12 , C07D401/14
摘要: Substituted biaryl quinolin-4-ylamine analogues of Formula I are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译: 提供式I的取代的联芳基喹啉-4-基胺类似物。 这些化合物是可用于在体内或体外调节特异性受体活性的配体,并且特别可用于治疗与人类,驯养伴侣动物和家畜中的病理受体激活相关的病症。 还提供了使用这些化合物治疗这种病症的药物组合物和方法,以及使用这些配体进行受体定位研究的方法。
-
公开(公告)号:US06403591B1
公开(公告)日:2002-06-11
申请号:US09894092
申请日:2001-06-28
IPC分类号: A61K31497
CPC分类号: C07D471/06 , C07D487/06 , G01N33/6896 , G01N33/9413 , G01N2333/70571 , G01N2800/2835
摘要: Disclosed are 1-Azatricyclic-4-benzylpiperazine compounds which are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.
摘要翻译: 公开了可用于治疗和/或预防神经心理障碍的1-叠氮基-4-苄基哌嗪化合物,包括但不限于精神分裂症,躁狂症,痴呆,抑郁,焦虑,强迫行为,药物滥用,帕金森氏样运动 与使用神经安定药相关的疾病和运动障碍。 还提供药物组合物,包括包装的药物组合物。 本发明的化合物也可用作组织样品中GABA A受体定位的探针。
-
公开(公告)号:US08580812B2
公开(公告)日:2013-11-12
申请号:US12595394
申请日:2008-04-09
申请人: David C. Ihle , Qin Guo , Kevin Hodgetts , Jun Yuan
发明人: David C. Ihle , Qin Guo , Kevin Hodgetts , Jun Yuan
IPC分类号: C07D221/02 , C07D491/02 , C07D498/02 , A01N43/42 , A61K31/44
CPC分类号: C07D471/04 , C07D455/02 , C07D471/10 , C07D498/10 , C07D519/00
摘要: Heteroaryl amide analogues are provided, of Formula (I), wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译: 提供了式(I)的杂芳基酰胺类似物,其中变量如本文所述。 这些化合物是可用于在体内或体外调节特异性受体活性的配体,并且特别可用于治疗与人类,驯养伴侣动物和家畜中的病理受体激活相关的病症。 还提供了使用这些化合物治疗这种病症的药物组合物和方法,以及使用这些配体进行受体定位研究的方法。
-
公开(公告)号:US20100266509A1
公开(公告)日:2010-10-21
申请号:US12595394
申请日:2008-04-09
申请人: David C. Ihle , Qin Guo , Kevin Hodgetts , Jun Yuan
发明人: David C. Ihle , Qin Guo , Kevin Hodgetts , Jun Yuan
IPC分类号: A61K31/5377 , C07D471/04 , A61K31/437 , C07D213/82 , A61K31/44 , C07D487/04 , A61K31/4985 , C07D413/14 , A61K31/519 , C07D401/14 , A61K31/497 , C07D498/10 , A61K31/438 , C07D403/14 , A61K9/12 , A61P29/00 , A61P25/00
CPC分类号: C07D471/04 , C07D455/02 , C07D471/10 , C07D498/10 , C07D519/00
摘要: Heteroaryl amide analogues are provided, of Formula (I), wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译: 提供了式(I)的杂芳基酰胺类似物,其中变量如本文所述。 这些化合物是可用于在体内或体外调节特异性受体活性的配体,并且特别可用于治疗与人类,驯养伴侣动物和家畜中的病理受体激活相关的病症。 还提供了使用这些化合物治疗这种病症的药物组合物和方法,以及使用这些配体进行受体定位研究的方法。
-
-
-
-
-
-
-
-
-