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：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：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：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：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：US20110263560A1

公开(公告)日：2011-10-27

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 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： A61K31/4523 ,  C07D401/10 ,  C07D401/12 ,  C07D413/12 ,  C07D413/04 ,  A61P9/12 ,  C07D417/12 ,  A61K31/451 ,  A61K31/4545 ,  A61K31/454 ,  A61K31/538 ,  A61K31/5415 ,  C07D211/60 ,  C07D405/12

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：US20100029647A1

公开(公告)日：2010-02-04

申请号：US11722398

申请日：2006-01-12

申请人： Keiichi Masuya ,  Osamu Irie ,  Atsuko Nihonyanagi ,  Atsushi Toyao ,  Takanori Kanazawa

发明人： Keiichi Masuya ,  Osamu Irie ,  Atsuko Nihonyanagi ,  Atsushi Toyao ,  Takanori Kanazawa

IPC分类号： A61K31/5377 ,  C07D401/12 ,  C07D213/56 ,  C07D413/12 ,  A61K31/4439 ,  A61K31/4406

CPC分类号： C07D401/12 ,  C07D211/78 ,  C07D401/10 ,  C07D409/12

摘要： 3,4(,5)-substituted tetrahydropyridine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease 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 tetrahydropyridine compound, and/or a method of treatment comprising administering a 3,4(,5)-substituted tetrahydropyridine compound, a method for the manufacture of a 3,4(,5)-substituted tetrahydropyridine compound, and novel intermediates and partial steps for its synthesis.The 3,4(,5)-substituted tetrahydropyridine compounds have the formula I wherein the substituents and symbols are as described in the specification.

摘要翻译： 3,4（，5） - 取代的四氢吡啶化合物，用于诊断和治疗温血动物的化合物，特别是用于治疗依赖于肾素活性的疾病; 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） - 取代四氢吡啶化合物的药物制剂和/或包括施用3,4（，5） - 取代的四氢吡啶化合物的方法， 5） - 取代的四氢吡啶化合物，以及其合成的新型中间体和部分步骤。 3,4（，5） - 取代的四氢吡啶化合物具有式I，其中取代基和符号如说明书中所述。

公开(公告)号：US20080242662A1

公开(公告)日：2008-10-02

申请号：US11915673

申请日：2006-05-29

申请人： Atsuko Nihonyanagi ,  Atsushi Toyao ,  Yuki Iwaki ,  Keiichi Masuya

发明人： Atsuko Nihonyanagi ,  Atsushi Toyao ,  Yuki Iwaki ,  Keiichi Masuya

IPC分类号： A61K31/495 ,  C07D241/04 ,  C07D403/12 ,  A61K31/538 ,  A61P43/00 ,  A61K31/496 ,  C07D265/36

CPC分类号： C07D417/14 ,  C07D403/12

摘要： The invention relates to substituted 3,4- or higher substituted piperazine compounds, the use thereof 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; 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; pharmaceutical formulations or products comprising said compounds, and/or a method of treatment comprising administering said compounds, a method for the manufacture of said compounds as well as novel intermediates, starting materials and/or partial steps for their synthesis. The compounds are especially of the formula I, wherein R1, R2, R11, C, E and D are as defined in the specification.

摘要翻译： 本发明涉及取代的3,4-或更高级取代的哌嗪化合物，其用于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; 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）; 药物制剂或包含所述化合物的产品，和/或包括施用所述化合物的处理方法，制备所述化合物的方法以及新型中间体，起始材料和/或其合成的部分步骤。 化合物特别是式I，其中R 1，R 2，R 11，C，E和D如说明书中所定义。

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.