公开(公告)号：US20060211747A1

公开(公告)日：2006-09-21

申请号：US11226786

申请日：2005-09-14

申请人： Pascal Furet ,  Francesco Hofmann ,  Edgar Jacoby ,  Joseph Schoepfer

发明人： Pascal Furet ,  Francesco Hofmann ,  Edgar Jacoby ,  Joseph Schoepfer

IPC分类号： A61K31/43

CPC分类号： A61K31/43

摘要： The present invention relates to methods of searching/screening for compounds which inhibit the activity of the ubiquitin conjugating enzyme Cdc34 in a zinc-mediated manner, to compounds obtainable by such a method, to a method of treating mammalian subjects with such compounds, to pharmaceutical compositions containing such compounds, to the use of such compounds for the treatment of diseases which respond to an inhibition of the activity of Cdc34 such as proliferative diseases, especially tumor diseases, and to the use of such compounds for the preparation of such pharmaceutical compositions for the treatment of such diseases.

摘要翻译： 本发明涉及以锌介导的方式检测/筛选抑制泛素缀合酶Cdc34的活性的化合物，通过这种方法可获得的化合物，将这些化合物治疗哺乳动物受试者的方法用于药物 含有这些化合物的组合物，用于这些化合物用于治疗对抑制Cdc34的活性（例如增殖性疾病，特别是肿瘤疾病）起反应的疾病，以及使用这些化合物制备这种药物组合物 治疗这种疾病。

公开(公告)号：US08440693B2

公开(公告)日：2013-05-14

申请号：US12973474

申请日：2010-12-20

申请人： Joerg Berghausen ,  Nicole Buschmann ,  Pascal Furet ,  François Gessier ,  Joanna Hergovich Lisztwan ,  Philipp Holzer ,  Edgar Jacoby ,  Joerg Kallen ,  Keiichi Masuya ,  Carole Pissot Soldermann ,  Haixia Ren ,  Stefan Stutz

发明人： Joerg Berghausen ,  Nicole Buschmann ,  Pascal Furet ,  François Gessier ,  Joanna Hergovich Lisztwan ,  Philipp Holzer ,  Edgar Jacoby ,  Joerg Kallen ,  Keiichi Masuya ,  Carole Pissot Soldermann ,  Haixia Ren ,  Stefan Stutz

IPC分类号： A01N37/18 ,  A61K31/65 ,  C07D215/00

CPC分类号： C07D239/82 ,  C07D217/24 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

摘要： The invention relates to substituted nitrogen containing bicyclic heterocycles of the formula (I) wherein Z is CH2 or N—R4 and X, R1, R2, R4, R6, R7 and n are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.

摘要翻译： 本发明涉及式（I）的取代的含氮双环杂环，其中Z是CH 2或N-R 4，X，R 1，R 2，R 4，R 6，R 7和n如说明书中所定义。 这些化合物适用于治疗由MDM2和/或MDM4或其变体的活性介导的病症或疾病。

公开(公告)号：US09649314B2

公开(公告)日：2017-05-16

申请号：US14652102

申请日：2013-12-12

申请人： Edgar Jacoby ,  Juergen Reinhardt ,  Niko Schmiedeberg ,  Carsten Spanka

发明人： Edgar Jacoby ,  Juergen Reinhardt ,  Niko Schmiedeberg ,  Carsten Spanka

IPC分类号： A61K31/519 ,  C07D471/14 ,  C07D471/04

CPC分类号： A61K31/519 ,  C07D471/04 ,  C07D471/14

摘要： The invention relates to compound of the formula (I); or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.

公开(公告)号：US20100087427A1

公开(公告)日：2010-04-08

申请号：US11721457

申请日：2005-12-21

申请人： Werner Breitenstein ,  Sylvain Cottens ,  Claus Ehrhardt ,  Edgar Jacoby ,  Edwige L. Lorthiolis ,  Juergen K. Maibaum ,  Nils Ostermann ,  Holger Sellner ,  Oliver Simic

发明人： Werner Breitenstein ,  Sylvain Cottens ,  Claus Ehrhardt ,  Edgar Jacoby ,  Edwige L. Lorthiolis ,  Juergen K. Maibaum ,  Nils Ostermann ,  Holger Sellner ,  Oliver Simic

IPC分类号： A61K31/538 ,  C07D207/50 ,  C07D403/12 ,  C07D417/12 ,  C07D413/12 ,  A61K31/40 ,  A61K31/4184 ,  A61K31/428 ,  A61P43/00

CPC分类号： C07D207/08 ,  C07D207/09 ,  C07D207/14 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D491/10

摘要： Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine 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 inappropriate 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 inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula I wherein the substituents are as described in the specification.

摘要翻译： 新型3-单，3,4-二和3,4,4-三取代的吡咯烷化合物，用于诊断和治疗温血动物，特别是用于治疗疾病的化合物 （=无序），取决于肾素的不适当活动; 使用该类化合物制备用于治疗依赖于肾素不适当活性的疾病的药物制剂; 使用该类化合物治疗依赖肾素不适当活动的疾病; 包括所述取代的吡咯烷化合物的药物制剂和/或包括施用所述取代的吡咯烷化合物的方法，制备所述取代的吡咯烷化合物的方法和新的中间体及其合成的部分步骤。 取代的吡咯烷化合物特别是式I，其中取代基如说明书中所述。

公开(公告)号：US08163773B2

公开(公告)日：2012-04-24

申请号：US11995484

申请日：2006-07-10

申请人： Werner Breitenstein ,  Claus Erhardt ,  Juergen Klaus Maibaum ,  Nils Ostermann ,  Juerg Zimmermann ,  Keiichi Masuya ,  Kazuhide Konishi ,  Fumiaki Yokokawa ,  Takanori Kanazawa ,  Edgar Jacoby ,  Andreas Marzinzik ,  Philipp Grosche ,  Shimpei Kawakami

发明人： Werner Breitenstein ,  Claus Erhardt ,  Juergen Klaus Maibaum ,  Nils Ostermann ,  Juerg Zimmermann ,  Keiichi Masuya ,  Kazuhide Konishi ,  Fumiaki Yokokawa ,  Takanori Kanazawa ,  Edgar Jacoby ,  Andreas Marzinzik ,  Philipp Grosche ,  Shimpei Kawakami

IPC分类号： A61K31/445 ,  C07D401/00

CPC分类号： C07D403/14 ,  C07D211/56 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

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 preferred compounds (which can also be present as salts) 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。 优选的化合物（其也可以盐形式存在）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：US20090233920A1

公开(公告)日：2009-09-17

申请号：US11995484

申请日：2006-07-10

申请人： Werner Breitenstein ,  Claus Erhardt ,  Juergen Klaus Maibaum ,  Nils Ostermann ,  Juerg Zimmermann ,  Keiichi Masuya ,  Kazuhide Konishi ,  Fumiaki Yokokawa ,  Takanori Kanazawa ,  Edgar Jacoby ,  Andreas Marzinzik ,  Philipp Grosche ,  Shimpei Kawakami

发明人： Werner Breitenstein ,  Claus Erhardt ,  Juergen Klaus Maibaum ,  Nils Ostermann ,  Juerg Zimmermann ,  Keiichi Masuya ,  Kazuhide Konishi ,  Fumiaki Yokokawa ,  Takanori Kanazawa ,  Edgar Jacoby ,  Andreas Marzinzik ,  Philipp Grosche ,  Shimpei Kawakami

IPC分类号： A61K31/538 ,  C07D265/36 ,  A61P9/12

CPC分类号： C07D403/14 ,  C07D211/56 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

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 preferred compounds (which can also be present as salts) 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。 优选的化合物（其也可以盐形式存在）具有式I，其中R 1，R 2，T，R 3和R 4如说明书中所定义。