公开(公告)号：US07074799B2

公开(公告)日：2006-07-11

申请号：US10347210

申请日：2003-01-17

申请人： Rajagopal Bakthavatchalam ,  Charles A. Blum ,  Harry Brielmann ,  Timothy M. Caldwell ,  Stephane De Lombaert ,  Kevin J. Hodgetts ,  Xiaozhang Zheng

发明人： Rajagopal Bakthavatchalam ,  Charles A. Blum ,  Harry Brielmann ,  Timothy M. Caldwell ,  Stephane De Lombaert ,  Kevin J. Hodgetts ,  Xiaozhang Zheng

IPC分类号： C07D403/12 ,  C07D403/14 ,  A61K31/519 ,  A61P3/04

CPC分类号： C07D401/04 ,  C07D215/42 ,  C07D215/44 ,  C07D237/34 ,  C07D239/94 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D419/14 ,  C07D471/04

摘要： Substituted quinazolin-4-ylamine analogues 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 them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

摘要翻译： 提供了取代的喹唑啉-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：US07432275B2

公开(公告)日：2008-10-07

申请号：US10539031

申请日：2003-12-12

申请人： Rajagopal Bakthavatchalam ,  Charles A. Blum ,  Harry Brielmann ,  Timothy M. Caldwell ,  Stéphane DeLombaert ,  Kevin J. Hodgetts ,  Xiaozhang Zheng

发明人： Rajagopal Bakthavatchalam ,  Charles A. Blum ,  Harry Brielmann ,  Timothy M. Caldwell ,  Stéphane DeLombaert ,  Kevin J. Hodgetts ,  Xiaozhang Zheng

IPC分类号： A01N43/54 ,  A61K31/517 ,  C07D239/72

CPC分类号： C07D417/14 ,  C07D239/94 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  C07D491/10 ,  C07F9/65128 ,  C07F9/65583 ,  C07F9/6561

摘要： Acid-substituted quinazolin-4-ylamine analogues 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 them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

摘要翻译： 提供了酸取代的喹唑啉-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：US07304059B2

公开(公告)日：2007-12-04

申请号：US11345926

申请日：2006-02-01

申请人： Rajagopal Bakthavatchalam ,  Charles A. Blum ,  Harry Brielmann ,  Timothy M. Caldwell ,  Stéphane De Lombaert ,  Kevin J. Hodgetts ,  Xiaozhang Zheng ,  Taeyoung Yoon

发明人： Rajagopal Bakthavatchalam ,  Charles A. Blum ,  Harry Brielmann ,  Timothy M. Caldwell ,  Stéphane De Lombaert ,  Kevin J. Hodgetts ,  Xiaozhang Zheng ,  Taeyoung Yoon

IPC分类号： C07D403/12 ,  C07D403/14 ,  A61K31/517

CPC分类号： C07D401/04 ,  C07D215/42 ,  C07D215/44 ,  C07D237/34 ,  C07D239/94 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D419/14 ,  C07D471/04

摘要： Substituted quinazolin-4-ylamine analogues 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 them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

摘要翻译： 提供了取代的喹唑啉-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：US20080153857A1

公开(公告)日：2008-06-26

申请号：US11953858

申请日：2007-12-10

申请人： Rajagopal Bakthavatchalam ,  Charles A. Blum ,  Harry Brielmann ,  Stephane De Lombaert ,  Xiaozhang Zheng

发明人： Rajagopal Bakthavatchalam ,  Charles A. Blum ,  Harry Brielmann ,  Stephane De Lombaert ,  Xiaozhang Zheng

IPC分类号： A61K31/519 ,  C07D401/04 ,  C07D401/14 ,  C12N5/00 ,  A61P3/04 ,  A61P43/00 ,  A61P25/00 ,  C07D471/04 ,  A61K31/506

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/14

摘要： Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues 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 them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

摘要翻译： 提供了取代的（7-吡啶基-4-苯基氨基 - 喹唑啉-2-基） - 甲醇类似物。 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：US20080015183A1

公开(公告)日：2008-01-17

申请号：US11864987

申请日：2007-09-29

申请人： Rajagopal Bakthavatchalam ,  Charles Blum ,  Harry Brielmann ,  Timothy Caldwell ,  Stephane De Lombaert ,  Kevin Hodgetts ,  Xiaozhang Zheng ,  James Krause ,  Uri Herzberg ,  Taeyoung Yoon

发明人： Rajagopal Bakthavatchalam ,  Charles Blum ,  Harry Brielmann ,  Timothy Caldwell ,  Stephane De Lombaert ,  Kevin Hodgetts ,  Xiaozhang Zheng ,  James Krause ,  Uri Herzberg ,  Taeyoung Yoon

IPC分类号： A61K31/517 ,  A61K31/47 ,  A61K31/519 ,  A61K31/541 ,  A61P11/14 ,  A61P17/02 ,  C07D215/58 ,  C07D237/30 ,  C07D279/12 ,  C07D471/04 ,  C07D417/12 ,  C07D413/14 ,  C07D413/10 ,  C07D401/14 ,  C07D401/10 ,  C07D239/84 ,  C07D223/04 ,  A61P25/04 ,  A61P11/16 ,  A61K31/55 ,  A61K31/5377 ,  A61K31/502

CPC分类号： C07D401/04 ,  C07D215/42 ,  C07D215/44 ,  C07D237/34 ,  C07D239/94 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D419/14 ,  C07D471/04

摘要： Substituted quinazolin-4-ylamine analogues 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 them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

摘要翻译： 提供了取代的喹唑啉-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：US20060173003A1

公开(公告)日：2006-08-03

申请号：US11345926

申请日：2006-02-01

申请人： Rajagopal Bakthavatchalam ,  Charles Blum ,  Harry Brielmann ,  Timothy Caldwell ,  Stephane De Lombaert ,  Kevin Hodgetts ,  Xiaozhang Zheng ,  James Krause ,  Uri Herzberg

发明人： Rajagopal Bakthavatchalam ,  Charles Blum ,  Harry Brielmann ,  Timothy Caldwell ,  Stephane De Lombaert ,  Kevin Hodgetts ,  Xiaozhang Zheng ,  James Krause ,  Uri Herzberg

IPC分类号： A61K31/5377 ,  A61K31/519 ,  A61K31/517 ,  C07D413/02 ,  C07D487/02 ,  C07D403/02

CPC分类号： C07D401/04 ,  C07D215/42 ,  C07D215/44 ,  C07D237/34 ,  C07D239/94 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D419/14 ,  C07D471/04

摘要： Substituted quinazolin-4-ylamine analogues 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 them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

公开(公告)号：US20050215575A1

公开(公告)日：2005-09-29

申请号：US10892741

申请日：2004-07-16

申请人： Rajagopal Bakthavatchalam ,  Charles Blum ,  Harry Brielmann ,  Stephane De Lombaert ,  Xiaozhang Zheng

发明人： Rajagopal Bakthavatchalam ,  Charles Blum ,  Harry Brielmann ,  Stephane De Lombaert ,  Xiaozhang Zheng

IPC分类号： A61K31/517 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D43/02

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/14

摘要： Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues 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 them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

摘要翻译： 提供了取代的（7-吡啶基-4-苯基氨基 - 喹唑啉-2-基） - 甲醇类似物。 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：US20050033048A1

公开(公告)日：2005-02-10

申请号：US10415457

申请日：2001-12-11

申请人： Rajagopal Bakthavatchalam ,  Charles Blum ,  Harry Brielmann ,  James Darrow ,  Stephane De Lombaert ,  Alan Hutchison ,  Jennifer Tran ,  Xiaozhang Zheng ,  Richard Elliott ,  Marlys Hammond

发明人： Rajagopal Bakthavatchalam ,  Charles Blum ,  Harry Brielmann ,  James Darrow ,  Stephane De Lombaert ,  Alan Hutchison ,  Jennifer Tran ,  Xiaozhang Zheng ,  Richard Elliott ,  Marlys Hammond

IPC分类号： C07D491/107 ,  A61K31/438 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K51/00 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  A61P43/00 ,  C07D487/04 ,  C07D487/10 ,  C07D491/10 ,  C07D519/00

CPC分类号： C07D487/04 ,  C07D491/10

摘要： Substituted spiro[isobenzofuran-1,4′-piperidin]-3-ones and 3H-spiroisobenzofuran-1,4′-piperidines capable of modulating NPY5 receptor activity are provided. Such compounds may be used to modulate ligand binding to NPY5 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders (e.g., eating disorders such as obesity or bulimia, psychiatric disorders, diabetes and cardiovascular disorders such as hypertension) in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and method for treating such disorders are provided, as are methods for using such compounds for detecting NPY5 receptors.

摘要翻译： 提供了能够调节NPY5受体活性的取代螺[异苯并呋喃-1,4'-哌啶] -3-酮和3H-螺异苯并呋喃-1,4'-哌啶。 这样的化合物可用于在体内或体外调节配体与NPY5受体的结合，并且特别可用于治疗多种疾病（例如，进食障碍，例如肥胖或贪食症，精神疾病，糖尿病和心血管疾病，例如 高血压），驯养的伴侣动物和家畜。 还提供了用于治疗这种病症的药物组合物和方法，以及使用这些化合物检测NPY5受体的方法。

公开(公告)号：US20070027155A1

公开(公告)日：2007-02-01

申请号：US10893799

申请日：2004-07-16

申请人： Rajagopal Bakthavatchalam ,  Charles Blum ,  Harry Brielmann ,  Bertrand Chenard ,  Stephane De Lombaert ,  Kevin Hodgetts ,  Alan Hutchison ,  Taeyoung Yoon ,  Xiaozhang Zheng

发明人： Rajagopal Bakthavatchalam ,  Charles Blum ,  Harry Brielmann ,  Bertrand Chenard ,  Stephane De Lombaert ,  Kevin Hodgetts ,  Alan Hutchison ,  Taeyoung Yoon ,  Xiaozhang Zheng

IPC分类号： A61K31/53 ,  A61K31/506 ,  C07D43/14

CPC分类号： C04B35/632 ,  A61K31/496 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  C07D251/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14

摘要： Biaryl piperazinyl-pyridine analogues are provided, of the Formula: 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： 提供了下式的双芳基哌嗪基 - 吡啶类似物：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：US20060040964A1

公开(公告)日：2006-02-23

申请号：US11183615

申请日：2005-07-18

申请人： Rajagopal Bakthavatchalam ,  Charles Blum ,  Harry Brielmann ,  James Darrow ,  Stephane De Lombaert ,  Alan Hutchison ,  Jennifer Tran ,  Xiaozhang Zheng ,  Richard Elliott ,  Marlys Hammond

发明人： Rajagopal Bakthavatchalam ,  Charles Blum ,  Harry Brielmann ,  James Darrow ,  Stephane De Lombaert ,  Alan Hutchison ,  Jennifer Tran ,  Xiaozhang Zheng ,  Richard Elliott ,  Marlys Hammond

IPC分类号： A61K31/519 ,  A61K31/4747 ,  C07D491/10

CPC分类号： C07D487/04 ,  C07D491/10

摘要： Substituted spiro[isobenzofuran-1,4′-piperidin]-3-ones and 3H-spiroisobenzofuran-1,4′-piperidines capable of modulating NPY5 receptor activity are provided. Such compounds may be used to modulate ligand binding to NPY5 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders (e.g., eating disorders such as obesity or bulimia, psychiatric disorders, diabetes and cardiovascular disorders such as hypertension) in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such compounds for detecting NPY5 receptors.