公开(公告)号：US08497286B2

公开(公告)日：2013-07-30

申请号：US13616081

申请日：2012-09-14

申请人： Fumiaki Yokokawa ,  Takeru Ehara ,  Shimpei Kawakami ,  Osamu Irie ,  Masaki Suzuki ,  Yuko Hitomi ,  Atsushi Toyao

发明人： Fumiaki Yokokawa ,  Takeru Ehara ,  Shimpei Kawakami ,  Osamu Irie ,  Masaki Suzuki ,  Yuko Hitomi ,  Atsushi Toyao

IPC分类号： A61K31/444 ,  C07D211/32

CPC分类号： C07D401/12

摘要： The present invention relates to a compound of the formula I wherein R1, R2, R3, R4 and R5 are as defined in the specification, for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations a compound of that class; a method of treatment comprising administering a compound of that class and a method for its manufacture.

摘要翻译： 本发明涉及式I化合物，其中R1，R2，R3，R4和R5如说明书中所定义，用于诊断和治疗温血动物，特别是用于治疗疾病 （=无效），依赖于肾素的活性; 使用该类化合物制备用于治疗依赖于肾素活性的疾病的药物制剂; 使用该类化合物治疗依赖于肾素活性的疾病; 药物制剂是该类化合物; 一种治疗方法，包括施用该类化合物及其制备方法。

公开(公告)号：US08383650B2

公开(公告)日：2013-02-26

申请号：US12146073

申请日：2008-06-25

申请人： Fumiaki Yokokawa ,  Takeru Ehara ,  Shimpei Kawakami ,  Osamu Irie ,  Masaki Suzuki ,  Yuko Hitomi ,  Atsushi Toyao

发明人： Fumiaki Yokokawa ,  Takeru Ehara ,  Shimpei Kawakami ,  Osamu Irie ,  Masaki Suzuki ,  Yuko Hitomi ,  Atsushi Toyao

IPC分类号： C07D401/12 ,  A61K31/4545 ,  A61P9/12 ,  A61P9/04 ,  A61P9/10 ,  A61P13/12 ,  A61P25/22 ,  A61P25/28 ,  A61P27/06

CPC分类号： C07D401/12

摘要： The present invention relates to a compound of the formula I wherein R1, R2, R3, R4 and R5 are as defined in the specification, for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations a compound of that class; a method of treatment comprising administering a compound of that class and a method for its manufacture.

公开(公告)号：US20130005770A1

公开(公告)日：2013-01-03

申请号：US13616081

申请日：2012-09-14

申请人： Fumiaki Yokokawa ,  Takeru Ehara ,  Shimpei Kawakami ,  Osamu Irie ,  Masaki Suzuki ,  Yuko Hitomi ,  Atsushi Toyao

发明人： Fumiaki Yokokawa ,  Takeru Ehara ,  Shimpei Kawakami ,  Osamu Irie ,  Masaki Suzuki ,  Yuko Hitomi ,  Atsushi Toyao

IPC分类号： A61K31/4545 ,  A61P9/12 ,  A61P9/10 ,  A61P9/04 ,  A61P27/02 ,  A61P13/12 ,  A61P1/16 ,  A61P25/28 ,  A61P25/22 ,  C07D401/12 ,  A61P9/00

CPC分类号： C07D401/12

摘要： The present invention relates to a compound of the formula I wherein R1, R2, R3, R4 and R5 are as defined in the specification, for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations a compound of that class; a method of treatment comprising administering a compound of that class and a method for its manufacture.

摘要翻译： 本发明涉及式I化合物，其中R1，R2，R3，R4和R5如说明书中所定义，用于诊断和治疗温血动物，特别是用于治疗疾病 （=无效），依赖于肾素的活性; 使用该类化合物制备用于治疗依赖于肾素活性的疾病的药物制剂; 使用该类化合物治疗依赖于肾素活性的疾病; 药物制剂是该类化合物; 一种治疗方法，包括施用该类化合物及其制备方法。

公开(公告)号：US20080319018A1

公开(公告)日：2008-12-25

申请号：US12146073

申请日：2008-06-25

申请人： Fumiaki Yokokawa ,  Takeru Ehara ,  Shimpei Kawakami ,  Osamu Irie ,  Masaki Suzuki ,  Yuku Hitomi ,  Atsushi Toyao

发明人： Fumiaki Yokokawa ,  Takeru Ehara ,  Shimpei Kawakami ,  Osamu Irie ,  Masaki Suzuki ,  Yuku Hitomi ,  Atsushi Toyao

IPC分类号： A61K31/4545 ,  C07D401/12 ,  A61P43/00

CPC分类号： C07D401/12

摘要： The present invention relates to a compound of the formula I wherein R1, R2, R3, R4 and R5 are as defined in the specification, for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations a compound of that class; a method of treatment comprising administering a compound of that class and a method for its manufacture.

摘要翻译： 本发明涉及式I化合物，其中R1，R2，R3，R4和R5如说明书中所定义，用于诊断和治疗温血动物，特别是用于治疗疾病 （=无效），依赖于肾素的活性; 使用该类化合物制备用于治疗依赖于肾素活性的疾病的药物制剂; 使用该类化合物治疗依赖于肾素活性的疾病; 药物制剂是该类化合物; 一种治疗方法，包括施用该类化合物及其制备方法。

公开(公告)号：US20090312304A1

公开(公告)日：2009-12-17

申请号：US11719762

申请日：2005-12-28

申请人： Werner Breitenstein ,  Takeru Ehara ,  Claus Ehrhardt ,  Philipp Grosche ,  Yuko Hitomi ,  Yuki Iwaki ,  Takanori Kanazawa ,  Kazuhide Konishi ,  Juergen K. Maibaum ,  Keiichi Masuya ,  Atsuko Nihonyanagi ,  Nils Ostermann ,  Masaki Suzuki ,  Atsushi Toyao ,  Fumiaki Yokokawa

发明人： Werner Breitenstein ,  Takeru Ehara ,  Claus Ehrhardt ,  Philipp Grosche ,  Yuko Hitomi ,  Yuki Iwaki ,  Takanori Kanazawa ,  Kazuhide Konishi ,  Juergen K. Maibaum ,  Keiichi Masuya ,  Atsuko Nihonyanagi ,  Nils Ostermann ,  Masaki Suzuki ,  Atsushi Toyao ,  Fumiaki Yokokawa

IPC分类号： A61K31/4545 ,  C07D211/00 ,  C07D401/10 ,  C07D413/12 ,  C07D417/12 ,  A61K31/445 ,  A61K31/536 ,  A61K31/5415

CPC分类号： C07D471/04 ,  C07D211/60 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/10 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

摘要： 3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4-substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula I,

摘要翻译： 3,4-取代的哌啶化合物，这些化合物用于诊断和治疗温血动物，特别是用于治疗依赖于肾素活性的疾病（=病症）; 使用该类化合物制备用于治疗依赖于肾素活性的疾病的药物制剂; 使用该类化合物治疗依赖于肾素活性的疾病; 包括3,4-取代的哌啶化合物的药物制剂和/或包括给药3,4-取代的哌啶化合物的方法，制备3,4-取代的哌啶化合物的方法和新的中间体和部分 公开了它们合成的步骤。 3,4-二取代的哌啶化合物具有式I，

公开(公告)号：US08084450B2

公开(公告)日：2011-12-27

申请号：US11719762

申请日：2005-12-28

申请人： Werner Breitenstein ,  Takeru Ehara ,  Claus Ehrhardt ,  Philipp Grosche ,  Yuko Hitomi ,  Yuki Iwaki ,  Takanori Kanazawa ,  Kazuhide Konishi ,  Juergen Klaus Maibaum ,  Keiichi Masuya ,  Atsuko Nihonyanagi ,  Nils Ostermann ,  Masaki Suzuki ,  Atsushi Toyao ,  Fumiaki Yokokawa

发明人： Werner Breitenstein ,  Takeru Ehara ,  Claus Ehrhardt ,  Philipp Grosche ,  Yuko Hitomi ,  Yuki Iwaki ,  Takanori Kanazawa ,  Kazuhide Konishi ,  Juergen Klaus Maibaum ,  Keiichi Masuya ,  Atsuko Nihonyanagi ,  Nils Ostermann ,  Masaki Suzuki ,  Atsushi Toyao ,  Fumiaki Yokokawa

IPC分类号： A61K31/536 ,  A61K31/451 ,  C07D265/36 ,  C07D211/60

CPC分类号： C07D471/04 ,  C07D211/60 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/10 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

摘要： 3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4-substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula I,

摘要翻译： 3,4-取代的哌啶化合物，这些化合物用于诊断和治疗温血动物，特别是用于治疗依赖于肾素活性的疾病（=病症）; 使用该类化合物制备用于治疗依赖于肾素活性的疾病的药物制剂; 使用该类化合物治疗依赖于肾素活性的疾病; 包括3,4-取代的哌啶化合物的药物制剂和/或包括给药3,4-取代的哌啶化合物的方法，制备3,4-取代的哌啶化合物的方法和新的中间体和部分 公开了它们合成的步骤。 3,4-二取代的哌啶化合物具有式I，

公开(公告)号：US08178559B2

公开(公告)日：2012-05-15

申请号：US13176930

申请日：2011-07-06

申请人： Werner Breitenstein ,  Takeru Ehara ,  Claus Ehrhardt ,  Philipp Grosche ,  Yuko Hitomi ,  Yuki Iwaki ,  Takanori Kanazawa ,  Kazuhide Konishi ,  Juergen Klaus Maibaum ,  Keiichi Masuya ,  Atsuko Iwasaki ,  Nils Ostermann ,  Masaki Suzuki ,  Atsushi Toyao ,  Fumiaki Yokokawa

发明人： Werner Breitenstein ,  Takeru Ehara ,  Claus Ehrhardt ,  Philipp Grosche ,  Yuko Hitomi ,  Yuki Iwaki ,  Takanori Kanazawa ,  Kazuhide Konishi ,  Juergen Klaus Maibaum ,  Keiichi Masuya ,  Atsuko Iwasaki ,  Nils Ostermann ,  Masaki Suzuki ,  Atsushi Toyao ,  Fumiaki Yokokawa

IPC分类号： A61K31/451 ,  C07D211/60

CPC分类号： C07D471/04 ,  C07D211/60 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/10 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

摘要： 3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula (I), wherein the symbols have the meanings defined in the specification.

摘要翻译： 3,4-取代的哌啶化合物，这些化合物用于诊断和治疗温血动物，特别是用于治疗依赖于肾素活性的疾病（=病症）; 使用该类化合物制备用于治疗依赖于肾素活性的疾病的药物制剂; 使用该类化合物治疗依赖于肾素活性的疾病; 包含3,4-取代的哌啶化合物的药物制剂和/或包括给药3,4代哌啶化合物的方法，制备3,4-取代的哌啶化合物的方法和新的中间体和部分步骤 他们的合成被公开。 3,4-二取代的哌啶化合物具有式（I），其中符号具有说明书中定义的含义。

公开(公告)号：US08129411B2

公开(公告)日：2012-03-06

申请号：US12159749

申请日：2006-12-28

申请人： Takeru Ehara ,  Philipp Grosche ,  Osamu Irie ,  Yuki Iwaki ,  Takanori Kanazawa ,  Shimpei Kawakami ,  Kazuhide Konishi ,  Muneto Mogi ,  Masaki Suzuki ,  Fumiaki Yokokawa

发明人： Takeru Ehara ,  Philipp Grosche ,  Osamu Irie ,  Yuki Iwaki ,  Takanori Kanazawa ,  Shimpei Kawakami ,  Kazuhide Konishi ,  Muneto Mogi ,  Masaki Suzuki ,  Fumiaki Yokokawa

IPC分类号： A61K31/454 ,  C07D401/02

CPC分类号： C07D401/12 ,  C07D211/60 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04

摘要： The invention relates to 3,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,5-substituted piperidine compound, a method for the manufacture of a 3,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis.The compounds have the formula I′ wherein R1, R2, T, R3 and R4 are as defined in the specification.

摘要翻译： 本发明涉及3,5-取代的哌啶化合物，这些化合物用于诊断和治疗温血动物，特别是用于治疗依赖于肾素活性的疾病（=病症）; 使用该类化合物制备用于治疗依赖于肾素活性的疾病的药物制剂; 使用该类化合物治疗依赖于肾素活性的疾病; 包含3,5-取代的哌啶化合物的药物制剂和/或治疗方法，包括给予3,5-取代的哌啶化合物，制备3,5-取代的哌啶化合物的方法，以及新的中间体和部分 其合成步骤。 化合物具有式I'，其中R 1，R 2，T，R 3和R 4如说明书中所定义。

公开(公告)号：US20090192148A1

公开(公告)日：2009-07-30

申请号：US12159749

申请日：2006-12-28

申请人： Takeru Ehara ,  Philipp Grosche ,  Osamu Irie ,  Yuki Iwaki ,  Takanori Kanazawa ,  Shimpei Kawakami ,  Kazuhide Konishi ,  Muneto Mogi ,  Masaki Suzuki ,  Fumiaki Yokokawa

发明人： Takeru Ehara ,  Philipp Grosche ,  Osamu Irie ,  Yuki Iwaki ,  Takanori Kanazawa ,  Shimpei Kawakami ,  Kazuhide Konishi ,  Muneto Mogi ,  Masaki Suzuki ,  Fumiaki Yokokawa

IPC分类号： A61K31/536 ,  C07D401/02 ,  C07D265/36 ,  C07D471/04 ,  A61K31/4725 ,  A61P43/00 ,  A61K31/437 ,  C07D215/20 ,  A61K31/454

CPC分类号： C07D401/12 ,  C07D211/60 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04

摘要： The invention relates to 3,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,5-substituted piperidine compound, a method for the manufacture of a 3,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis.The compounds have the formula I′ wherein R1, R2, T, R3 and R4 areas defined in the specification.

摘要翻译： 本发明涉及3,5-取代的哌啶化合物，这些化合物用于诊断和治疗温血动物，特别是用于治疗依赖于肾素活性的疾病（=病症）; 使用该类化合物制备用于治疗依赖于肾素活性的疾病的药物制剂; 使用该类化合物治疗依赖于肾素活性的疾病; 包含3,5-取代的哌啶化合物的药物制剂和/或治疗方法，包括给予3,5-取代的哌啶化合物，制备3,5-取代的哌啶化合物的方法，以及新的中间体和部分 其合成步骤。 化合物具有式I'，其中在说明书中定义的R1，R2，T，R3和R4区域。

公开(公告)号：US20100160305A1

公开(公告)日：2010-06-24

申请号：US11908182

申请日：2006-03-07

申请人： Keiichi Masuya ,  Fumiaki Yokokawa ,  Osamu Irie ,  Atsuko Nihonyanagi ,  Takeru Ehara ,  Kazuhide Konishi ,  Takanori Kanazawa ,  Masaki Suzuki

发明人： Keiichi Masuya ,  Fumiaki Yokokawa ,  Osamu Irie ,  Atsuko Nihonyanagi ,  Takeru Ehara ,  Kazuhide Konishi ,  Takanori Kanazawa ,  Masaki Suzuki

IPC分类号： A61K31/451 ,  A61K31/538 ,  A61K31/454 ,  C07D413/12 ,  C07D401/12 ,  C07D211/60 ,  A61P43/00

CPC分类号： C07D401/12 ,  C07D211/60 ,  C07D413/12

摘要： 3,4,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4,5-substituted piperidine compound, a method for the manufacture of a 3,4,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis.The compounds are of the formula I, wherein the substitutents are as defined in the specification.

摘要翻译： 3,4,5-取代的哌啶化合物，这些化合物用于诊断和治疗温血动物，特别是用于治疗依赖于肾素活性的疾病（=病症）; 使用该类化合物制备用于治疗依赖于肾素活性的疾病的药物制剂; 使用该类化合物治疗依赖于肾素活性的疾病; 包含3,4,5-取代的哌啶化合物的药物制剂和/或治疗方法，包括给予3,4,5-取代的哌啶化合物，制备3,4,5-取代哌啶化合物的方法 ，以及其合成的新型中间体和部分步骤。 化合物是式I，其中取代基如说明书中所定义。