公开(公告)号：US06410548B1

公开(公告)日：2002-06-25

申请号：US09781373

申请日：2001-02-12

申请人： Ravi P. Nargund ,  Zhixiong Ye ,  Brenda L. Palucki ,  Raman K. Bakshi ,  Arthur A. Patchett ,  Leonardus H. T. Van Der Ploeg

发明人： Ravi P. Nargund ,  Zhixiong Ye ,  Brenda L. Palucki ,  Raman K. Bakshi ,  Arthur A. Patchett ,  Leonardus H. T. Van Der Ploeg

IPC分类号： A61K31438

摘要： Certain novel spiropiperidine compounds are agonists of melanocortin receptor(s) and are useful for the treatment, control or prevention of diseases and disorders responsive to the activation of melanocortin receptors. The compounds of the present invention are therefore useful for treatment of diseases and disorders such as obesity, diabetes, sexual dysfunction including erectile dysfunction and female sexual dysfunction.

公开(公告)号：US06350760B1

公开(公告)日：2002-02-26

申请号：US09585111

申请日：2000-06-01

申请人： Raman K. Bakshi ,  Khaled J. Barakat ,  Ravi P. Nargund ,  Brenda L. Palucki ,  Arthur A. Patchett ,  Iyassu Sebhat ,  Zhixiong Ye ,  Leonardus H. T. Van Der Ploeg

发明人： Raman K. Bakshi ,  Khaled J. Barakat ,  Ravi P. Nargund ,  Brenda L. Palucki ,  Arthur A. Patchett ,  Iyassu Sebhat ,  Zhixiong Ye ,  Leonardus H. T. Van Der Ploeg

IPC分类号： A61K3144

CPC分类号： C07D231/12 ,  A61K31/4725 ,  A61K31/4985 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

摘要： Certain novel substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction. Also provided are methods of treating sexual dysfunction with a compound that is a selective agonist of MC-4R over any other human melanocortin receptor.

摘要翻译： 某些新的取代的哌啶化合物是人类黑皮质素受体的激动剂，特别是人黑素皮质素-4受体（MC-4R）的选择性激动剂。 因此，它们可用于治疗，控制或预防对MC-4R的激活反应的疾病和病症，例如肥胖，糖尿病，性功能障碍，包括勃起功能障碍和女性性功能障碍。 还提供了使用作为MC-4R的选择性激动剂的化合物超过任何其它人类黑皮质素受体来治疗性功能障碍的方法。

公开(公告)号：US06294534B1

公开(公告)日：2001-09-25

申请号：US09329814

申请日：1999-06-10

申请人： Ravi P. Nargund ,  Brenda L. Palucki ,  Zhixiong Ye ,  Raman K. Bakshi ,  Arthur A. Patchett ,  Leonardus H. T. Van Der Ploeg

发明人： Ravi P. Nargund ,  Brenda L. Palucki ,  Zhixiong Ye ,  Raman K. Bakshi ,  Arthur A. Patchett ,  Leonardus H. T. Van Der Ploeg

IPC分类号： A61K3144

CPC分类号： C07K5/06139 ,  A61K38/00 ,  C07K5/06191

摘要： Certain novel spiropiperidine compounds are agonists of melanocortin receptor(s) and are useful for the treatment, control or prevention of diseases and disorders responsive to the activation of melanocortin receptors. The compounds of the present invention are therefore useful for treatment of diseases and disorders such as obesity, diabetes, sexual dysfunction including erectile dysfunction and female sexual dysfunction.

公开(公告)号：US06767915B2

公开(公告)日：2004-07-27

申请号：US10343040

申请日：2003-01-27

申请人： Raman K. Bakshi ,  Khaled J. Barakat ,  Yingjie Lai ,  Ravi P. Nargund ,  Brenda L. Palucki ,  Min K. Park ,  Iyassu K. Sebhat ,  Zhixiong Ye ,  Arthur A. Patchett

发明人： Raman K. Bakshi ,  Khaled J. Barakat ,  Yingjie Lai ,  Ravi P. Nargund ,  Brenda L. Palucki ,  Min K. Park ,  Iyassu K. Sebhat ,  Zhixiong Ye ,  Arthur A. Patchett

IPC分类号： A61K31445

CPC分类号： C07D211/62 ,  A61K31/445 ,  A61K31/451 ,  A61K31/454 ,  A61K31/4545 ,  C07D211/20 ,  C07D211/24 ,  C07D211/26 ,  C07D401/06 ,  C07D409/12 ,  C07D413/06 ,  C07D417/06 ,  C07D487/08 ,  C07D491/08

摘要： Certain novel 4-substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

摘要翻译： 某些新的4-取代的哌啶化合物是人类黑皮质素受体的激动剂，特别是人黑素皮质素-4受体（MC-4R）的选择性激动剂。 因此，它们可用于治疗，控制或预防对MC-4R的激活反应的疾病和病症，例如肥胖，糖尿病，性功能障碍，包括勃起功能障碍和女性性功能障碍。

公开(公告)号：US07414057B2

公开(公告)日：2008-08-19

申请号：US10526178

申请日：2003-09-05

申请人： Raman Kumar Bakshi ,  Ravi P. Nargund ,  Brenda L. Palucki ,  Min K. Park ,  Zhixiong Ye

发明人： Raman Kumar Bakshi ,  Ravi P. Nargund ,  Brenda L. Palucki ,  Min K. Park ,  Zhixiong Ye

IPC分类号： C07D401/12 ,  C07D403/12 ,  A61K31/453 ,  A61K31/4545 ,  A61P3/04 ,  A61P3/10

CPC分类号： C07D401/12 ,  C07D211/18 ,  C07D211/22 ,  C07D211/62 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08

摘要： Certain novel piperazine urea derivatives are agonists of the human melanocortin-4 receptor (MC-4R) and, in particular, are receptor-subtype selective agonists of MC-4R. They are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity and diabetes.

摘要翻译： 某些新型哌嗪脲衍生物是人类黑皮质素-4受体（MC-4R）的激动剂，特别是MC-4R的受体亚型选择性激动剂。 它们可用于治疗，控制或预防对MC-4R活化反应的疾病和病症，例如肥胖症和糖尿病。

公开(公告)号：US06458790B2

公开(公告)日：2002-10-01

申请号：US09812965

申请日：2001-03-20

申请人： Brenda L. Palucki ,  Khaled J. Barakat ,  Liangqin Guo ,  Yingjie Lai ,  Ravi P. Nargund ,  Min K. Park ,  Patrick G. Pollard ,  Iyassu K. Sebhat ,  Zhixiong Ye

发明人： Brenda L. Palucki ,  Khaled J. Barakat ,  Liangqin Guo ,  Yingjie Lai ,  Ravi P. Nargund ,  Min K. Park ,  Patrick G. Pollard ,  Iyassu K. Sebhat ,  Zhixiong Ye

IPC分类号： C07D40112

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D487/08

摘要： Certain novel substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment and control of obesity, diabetes, and sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

摘要翻译： 某些新的取代的哌啶化合物是人类黑皮质素受体的激动剂，特别是人黑素皮质素-4受体（MC-4R）的选择性激动剂。 因此，它们可用于治疗和控制肥胖症，糖尿病和性功能障碍，包括勃起功能障碍和女性性功能障碍。

公开(公告)号：US06472398B1

公开(公告)日：2002-10-29

申请号：US09812339

申请日：2001-03-20

申请人： Brenda L. Palucki ,  Ravi P. Nargund

发明人： Brenda L. Palucki ,  Ravi P. Nargund

IPC分类号： A61K31496

CPC分类号： C07D471/10 ,  A61K38/00 ,  C07K5/06139

摘要： Certain novel spiropiperidine derivatives of structural formula Ia wherein the substituents are as defined herein are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

摘要翻译： 某些结构式Ia的新型螺哌啶衍生物，其中取代基如本文所定义，是人黑皮质素受体的激动剂，特别是人黑皮质素-4受体（MC-4R）的选择性激动剂。 因此，它们可用于治疗，控制或预防对MC-4R的激活反应的疾病和病症，例如肥胖，糖尿病，性功能障碍，包括勃起功能障碍和女性性功能障碍。