公开(公告)号：US06943199B2

公开(公告)日：2005-09-13

申请号：US10410648

申请日：2003-04-09

申请人： Stéphane De Lombaert ,  Alan Hutchison ,  Xiaozhang Zheng

发明人： Stéphane De Lombaert ,  Alan Hutchison ,  Xiaozhang Zheng

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 ,  A61K3/438 ,  C07D401/04 ,  C07D471/10 ,  C07D471/22

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.

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：US06566367B2

公开(公告)日：2003-05-20

申请号：US10013846

申请日：2001-12-11

申请人： Rajagopal Bakthavatchalam ,  Charles A. Blum ,  Harry L. Brielmann ,  James William Darrow ,  Stéphane De Lombaert ,  Alan Hutchison ,  Jennifer Tran ,  Xiaozhang Zheng ,  Richard Louis Elliott ,  Marlys Hammond

发明人： Rajagopal Bakthavatchalam ,  Charles A. Blum ,  Harry L. Brielmann ,  James William Darrow ,  Stéphane De Lombaert ,  Alan Hutchison ,  Jennifer Tran ,  Xiaozhang Zheng ,  Richard Louis Elliott ,  Marlys Hammond

IPC分类号： C07D47110

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.

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.

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：US07323478B2

公开(公告)日：2008-01-29

申请号：US10820344

申请日：2004-04-08

申请人： Rajagopal Bakthavatchalam ,  Andrew Thurkauf ,  Alan Hutchison

发明人： Rajagopal Bakthavatchalam ,  Andrew Thurkauf ,  Alan Hutchison

IPC分类号： A61K31/445

CPC分类号： C07D295/096

摘要： Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein Q, X, Y, Z, and R1 R9, and R12-R19 are defined herein. These compounds are selective modulators of MCH 1 receptors that are, therefore, useful in the treatment of a variety of metabolic, feeding, and sexual disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also disclosed.

摘要翻译： 公开了下式的化合物及其药学上可接受的盐，其中Q，X，Y，Z和R 1 R 9和R 12， 本文定义了本文所述的方法。 这些化合物是MCH 1受体的选择性调节剂，因此可用于治疗各种代谢，喂养和性功能障碍。 还公开了治疗这种病症以及包装的药物组合物的方法。

公开(公告)号：US20070249616A1

公开(公告)日：2007-10-25

申请号：US11763926

申请日：2007-06-15

申请人： Alan Hutchison ,  Bertrand Chenard ,  James Tarrant ,  Guiying Li ,  Manuka Ghosh ,  George Luke ,  John Peterson ,  Wallace Pringle ,  Mary-Margaret O'Donnell ,  Kyungae Lee ,  Linda Gustavson ,  Dario Doller

发明人： Alan Hutchison ,  Bertrand Chenard ,  James Tarrant ,  Guiying Li ,  Manuka Ghosh ,  George Luke ,  John Peterson ,  Wallace Pringle ,  Mary-Margaret O'Donnell ,  Kyungae Lee ,  Linda Gustavson ,  Dario Doller

IPC分类号： A61K31/496 ,  A61K31/498 ,  A61P3/04

CPC分类号： C07D213/74 ,  C07D213/82 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08

摘要： Compounds of Formula I are provided, in which variables are as described herein: Such compounds may be used to modulate MCH binding to MCH receptors 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： 提供了式I化合物，其中变量如本文所述：这样的化合物可用于在体内或体外调节MCH与MCH受体的结合，并且特别可用于治疗各种代谢，进食和性障碍 在人类，驯养的伴侣动物和家畜中。 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：US07160879B2

公开(公告)日：2007-01-09

申请号：US10339499

申请日：2003-01-09

申请人： Robert W. DeSimone ,  John M. Peterson ,  Cheryl Steenstra ,  Yiping Shen ,  Linda M. Gustavson ,  Christopher Mach ,  Alan Hutchison

发明人： Robert W. DeSimone ,  John M. Peterson ,  Cheryl Steenstra ,  Yiping Shen ,  Linda M. Gustavson ,  Christopher Mach ,  Alan Hutchison

IPC分类号： A61P15/00 ,  A61K31/55 ,  A61K31/495 ,  C07D243/08 ,  C07D401/00

CPC分类号： C07D401/06 ,  C07D235/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14

摘要： Melanin concentrating hormone receptor ligands (especially substituted 2-(4-benzyl-piperazin-1-ylmethyl)-1H-benzoimidazole analogues), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors 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： 提供能够调节MCH受体活性的黑色素浓缩激素受体配体（特别是取代的2-（4-苄基 - 哌嗪-1-基甲基）-1H-苯并咪唑类似物）。 这样的配体可用于在体内或体外调节MCH与MCH受体的结合，并且特别可用于治疗人，驯养的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：US20060142324A1

公开(公告)日：2006-06-29

申请号：US11355439

申请日：2006-02-15

申请人： Jun Yuan ,  George Maynard ,  Alan Hutchison

发明人： Jun Yuan ,  George Maynard ,  Alan Hutchison

IPC分类号： A61K31/4745 ,  C07D471/02

CPC分类号： C07D471/04 ,  C07D495/04

摘要： Disclosed are compounds of formula (I) or pharmaceutically acceptable non-toxic salts or pharmaceutically acceptable solvates thereof wherein: (II) represents (a), (b), (c) or (d) and W, X, Y, A, B, C, D, E are variables as described herein. These compounds are highly selective agonists or antagonists at NK3 receptors or prodrugs thereof. The novel tachykinin NK-3 receptor antagonists contained in this invention have potential utility in the treatment of a broad array of disorders and diseases of the central nervous system (CNS) and periphery in mammals in which activation of NK-3 receptors is of importance.