公开(公告)号：US20100029687A1

公开(公告)日：2010-02-04

申请号：US12514869

申请日：2007-11-14

申请人： Shunichiro Hachiya ,  Kazuhiro Ikegai ,  Ryotaro Ibuka ,  Taisuke Takahashi ,  Makoto Oku ,  Ryushi Seo ,  Yoh Terada ,  Masanao Sanagi

发明人： Shunichiro Hachiya ,  Kazuhiro Ikegai ,  Ryotaro Ibuka ,  Taisuke Takahashi ,  Makoto Oku ,  Ryushi Seo ,  Yoh Terada ,  Masanao Sanagi

IPC分类号： A61K31/497 ,  C07D211/30 ,  C07D413/12 ,  C07D401/12 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/445 ,  A61P5/18

CPC分类号： C07D211/26 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D405/06 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07D417/06

摘要： [Problem] To provide a compound which can be used for treating diseases in which a calcium sensing receptor (CaSR) participates, particularly hyperparathyroidism.[Means for Resolution] It was found that a novel piperidine derivative which is characterized in that one of a 3-position and a 4-position is substituted with an aminomethyl group substituted with an arylalkyl group or the like and the other position is substituted with aryl, heteroaryl or the like, or a salt thereof, has an excellent CaSR agonistic regulatory action, and also has excellent selectivity with a CYP2D6 inhibitory action having a possibility of causing drug interaction. Based on the above, this novel piperidine derivative is useful as a therapeutic agent for diseases in which CaSR participates (hyperparathyroidism, renal osteodystrophy, hypercalcemia, and the like).

摘要翻译： [问题]提供可用于治疗钙感觉受体（CaSR）参与的疾病的化合物，特别是甲状旁腺功能亢进。 [解决方法]发现一种新的哌啶衍生物，其特征在于3-位和4-位中的一个被被芳基烷基等取代的氨基甲基取代，另一个位置被 芳基，杂芳基等，或其盐具有优异的CaSR激动调节作用，并且与具有引起药物相互作用的可能性的CYP2D6抑制作用也具有优异的选择性。 基于上述，该新型哌啶衍生物可用作CaSR参与的疾病（甲状旁腺功能亢进，肾性骨营养不良，高钙血症等）的治疗剂。

公开(公告)号：US08153658B2

公开(公告)日：2012-04-10

申请号：US12514869

申请日：2007-11-14

申请人： Shunichiro Hachiya ,  Kazuhiro Ikegai ,  Ryotaro Ibuka ,  Taisuke Takahashi ,  Makoto Oku ,  Ryushi Seo ,  Yoh Terada ,  Masanao Sanagi

发明人： Shunichiro Hachiya ,  Kazuhiro Ikegai ,  Ryotaro Ibuka ,  Taisuke Takahashi ,  Makoto Oku ,  Ryushi Seo ,  Yoh Terada ,  Masanao Sanagi

IPC分类号： A61K31/4525 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/4545 ,  C07D409/12 ,  C07D405/04 ,  C07D413/04 ,  C07D411/04 ,  C07D401/04 ,  C07D401/12

CPC分类号： C07D211/26 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D405/06 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07D417/06

摘要： To provide a compound which can be used for treating diseases in which a calcium sensing receptor (CaSR) participates, particularly hyperparathyroidism. It was found that a novel piperidine derivative which is characterized in that one of a 3-position and a 4-position is substituted with an aminomethyl group substituted with an arylalkyl group or the like and the other position is substituted with aryl, heteroaryl or the like, or a salt thereof, has an excellent CaSR agonistic regulatory action, and also has excellent selectivity with a CYP2D6 inhibitory action having a possibility of causing drug interaction. Based on the above, this novel piperidine derivative is useful as a therapeutic agent for diseases in which CaSR participates (hyperparathyroidism, renal osteodystrophy, hypercalcemia, and the like).

摘要翻译： 提供可用于治疗钙感觉受体（CaSR）参与的疾病的化合物，特别是甲状旁腺功能亢进。 发现新的哌啶衍生物，其特征在于3-位和4-位中的一个被被芳基烷基等取代的氨基甲基取代，另一个位置被芳基，杂芳基或 或其盐具有优异的CaSR激动调节作用，并且与具有引起药物相互作用的可能性的CYP2D6抑制作用也具有优异的选择性。 基于上述，该新型哌啶衍生物可用作CaSR参与的疾病（甲状旁腺功能亢进，肾性骨营养不良，高钙血症等）的治疗剂。

公开(公告)号：US20090062366A1

公开(公告)日：2009-03-05

申请号：US11662539

申请日：2006-05-18

申请人： Shunichiro Hachiya ,  Makoto Oku ,  Hana Mukai ,  Takashi Shin ,  Keisuke Matsuura ,  Ryushi Seo ,  Takashi Kamikubo ,  Yoh Terada ,  Masanao Sanagi ,  Kousei Yoshihara ,  Taisuke Takahashi

发明人： Shunichiro Hachiya ,  Makoto Oku ,  Hana Mukai ,  Takashi Shin ,  Keisuke Matsuura ,  Ryushi Seo ,  Takashi Kamikubo ,  Yoh Terada ,  Masanao Sanagi ,  Kousei Yoshihara ,  Taisuke Takahashi

IPC分类号： A61K31/40 ,  C07D207/04

CPC分类号： C07D207/09 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/10 ,  C07D417/06 ,  C07D417/10

摘要： [Problem] To provide a compound which may be used in treating diseases in which a calcium sensing receptor (CaSR) is concerned, particularly hyperparathyroidism.[Means for Resolution] It was found that novel pyrrolidine derivatives which are characterized by the possession of aminomethyl group substituted with arylalkyl group or the like, or salts thereof, have excellent CaSR agonistic regulatory activity and also have excellent selectivity with CYP2D6 inhibitory activity having a possibility of causing drug interaction. Based on the above, these novel pyrrolidine derivatives are useful as therapeutic agents for treating diseases in which CaSR is concerned (hyperparathyroidism, renal osteodystrophy, hypercalcemia and the like).

公开(公告)号：US07585886B2

公开(公告)日：2009-09-08

申请号：US11662539

申请日：2006-05-18

申请人： Shunichiro Hachiya ,  Makoto Oku ,  Hana Mukai ,  Takashi Shin ,  Keisuke Matsuura ,  Ryushi Seo ,  Takashi Kamikubo ,  Yoh Terada ,  Masanao Sanagi ,  Kousei Yoshihara ,  Taisuke Takahashi

发明人： Shunichiro Hachiya ,  Makoto Oku ,  Hana Mukai ,  Takashi Shin ,  Keisuke Matsuura ,  Ryushi Seo ,  Takashi Kamikubo ,  Yoh Terada ,  Masanao Sanagi ,  Kousei Yoshihara ,  Taisuke Takahashi

IPC分类号： C07D207/00 ,  A61K31/40

CPC分类号： C07D207/09 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/10 ,  C07D417/06 ,  C07D417/10

摘要： [Problem] To provide a compound which may be used in treating diseases in which a calcium sensing receptor (CaSR) is concerned, particularly hyperparathyroidism. [Means for Resolution] It was found that novel pyrrolidine derivatives which are characterized by the possession of aminomethyl group substituted with arylalkyl group or the like, or salts thereof, have excellent CaSR agonistic regulatory activity and also have excellent selectivity with CYP2D6 inhibitory activity having a possibility of causing drug interaction. Based on the above, these novel pyrrolidine derivatives are useful as therapeutic agents for treating diseases in which CaSR is concerned (hyperparathyroidism, renal osteodystrophy, hypercalcemia and the like).

摘要翻译： [问题]提供可用于治疗其中涉及钙感觉受体（CaSR）的疾病的化合物，特别是甲状旁腺机能亢进。 [解决方法]发现以芳基烷基等取代的氨甲基为特征的新型吡咯烷衍生物或其盐具有优异的CaSR激动调节活性，并且对于CYP2D6抑制活性也具有优异的选择性，具有 引起药物相互作用的可能性。 基于上述，这些新型吡咯烷衍生物可用作治疗涉及CaSR的疾病（甲状旁腺功能亢进，肾性骨营养不良，高钙血症等）的治疗剂。

公开(公告)号：US09108977B2

公开(公告)日：2015-08-18

申请号：US13613948

申请日：2012-09-13

申请人： Hiroyuki Koshio ,  Norio Asai ,  Taisuke Takahashi ,  Takafumi Shimizu ,  Yasuhito Nagai ,  Keiko Kawabata ,  Karl Bruce Thor

发明人： Hiroyuki Koshio ,  Norio Asai ,  Taisuke Takahashi ,  Takafumi Shimizu ,  Yasuhito Nagai ,  Keiko Kawabata ,  Karl Bruce Thor

IPC分类号： A61K31/55 ,  C07D471/04 ,  C07D498/04 ,  C07D487/04

CPC分类号： C07D498/04 ,  A61K31/55 ,  C07D471/04 ,  C07D487/04

摘要： Provided is a compound which is useful as an agent for treating or preventing 5-HT2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like. The present inventors have investigated compounds having a 5-HT2C receptor agonist activity and have found that the benzazepine compounds of the present invention have an excellent 5-HT2C receptor agonist activity, thereby completing the present invention. That is, the benzazepine compounds of the present invention have a 5-HT2C receptor agonist activity and can be used as an agent for treating or preventing 5-HT2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like.

摘要翻译： 本发明提供可用作治疗或预防5-HT 2C受体相关疾病，特别是尿失禁，尿失禁尿，尿失禁等尿失禁的药物的化合物，勃起功能障碍综合征等性功能障碍， 类似物，肥胖症等。 本发明人研究了具有5-HT 2C受体激动剂活性的化合物，并且发现本发明的苯并氮杂化合物具有优异的5-HT 2C受体激动剂活性，从而完成了本发明。 也就是说，本发明的苯并氮杂化合物具有5-HT 2C受体激动剂活性，可用作治疗或预防5-HT 2C受体相关疾病的药剂，特别是尿失禁，压力性尿失禁，压力性尿失禁，混合型 尿失禁等，性功能障碍如勃起功能障碍综合征等，肥胖等。

公开(公告)号：US20130012496A1

公开(公告)日：2013-01-10

申请号：US13583410

申请日：2011-03-11

申请人： Hiroyuki Koshio ,  Norio Asai ,  Taisuke Takahashi ,  Takafumi Shimizu ,  Yasuhito Nagai ,  Keiko Kawabata ,  Karl Bruce Thor

发明人： Hiroyuki Koshio ,  Norio Asai ,  Taisuke Takahashi ,  Takafumi Shimizu ,  Yasuhito Nagai ,  Keiko Kawabata ,  Karl Bruce Thor

IPC分类号： A61K31/55 ,  A61P13/10 ,  C07D487/04 ,  C07D498/04

CPC分类号： C07D498/04 ,  A61K31/55 ,  C07D471/04 ,  C07D487/04

摘要： Provided is a compound which is useful as an agent for treating or preventing 5-HT2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like. The present inventors have investigated compounds having a 5-HT2C receptor agonist activity and have found that the benzazepine compounds of the present invention have an excellent 5-HT2C receptor agonist activity, thereby completing the present invention. That is, the benzazepine compounds of the present invention have a 5-HT2C receptor agonist activity and can be used as an agent for treating or preventing 5-HT2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like.