公开(公告)号：US20070275962A1

公开(公告)日：2007-11-29

申请号：US10597120

申请日：2004-09-10

申请人： Anil Koul ,  Bert Klebl ,  Gerhard Muller ,  Andrea Missio ,  Wilfried Schwab ,  Doris Hafenbradl ,  Lars Neumann ,  Marc-Nicola Sommer ,  Stefan Muller ,  Edmund Hoppe ,  Achim Freisleben ,  Alexander Backes ,  Christian Hartung ,  Beatrice Felber ,  Birgit Zech ,  Ola Engkvist ,  Gyorgy Keri ,  Laszlo Orfi ,  Peter Banhegyi ,  Zoltan Greff ,  Zoltan Horvath ,  Zoltan Varga ,  Peter Marko ,  Janos Pato ,  Istvan Szabadkai ,  Zsolt Szekelyhid ,  Frigyes Waczek

发明人： Anil Koul ,  Bert Klebl ,  Gerhard Muller ,  Andrea Missio ,  Wilfried Schwab ,  Doris Hafenbradl ,  Lars Neumann ,  Marc-Nicola Sommer ,  Stefan Muller ,  Edmund Hoppe ,  Achim Freisleben ,  Alexander Backes ,  Christian Hartung ,  Beatrice Felber ,  Birgit Zech ,  Ola Engkvist ,  Gyorgy Keri ,  Laszlo Orfi ,  Peter Banhegyi ,  Zoltan Greff ,  Zoltan Horvath ,  Zoltan Varga ,  Peter Marko ,  Janos Pato ,  Istvan Szabadkai ,  Zsolt Szekelyhid ,  Frigyes Waczek

IPC分类号： C07D495/04 ,  A61P31/04 ,  C07D209/42 ,  C07D333/66 ,  C07D333/68 ,  C07D495/10 ,  C07D409/12 ,  C07D413/14 ,  C07D491/04 ,  C07D493/04

CPC分类号： C07D409/12 ,  C07D209/42 ,  C07D333/66 ,  C07D333/68 ,  C07D491/04 ,  C07D493/04 ,  C07D495/04 ,  C07D495/10

摘要： Described are heterobicyclic compounds such as 4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]thiopyran 3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]pyran-3-carboxylic acid amides, or benzo[b]thiophene-3-carboxylic acid amides and pharmaceutically acceptable salts thereof, the use of these derivatives for the prophylaxis and/or treatment of various diseases such as infectious diseases, including mycobacteriainduced infections and opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, as well as compositions containing at least one heterobicyclic compound and/or pharmaceutically acceptable salts thereof. Furthermore, reaction procedures for the synthesis of the heterobicyclic compound are disclosed.

摘要翻译： 描述的是杂双环化合物，例如4,5,6,7-四氢苯并[b]噻吩-3-羧酸酰胺，4,7-二氢-5H-噻吩并[2,3-c]噻喃-3-羧酸酰胺，4 ，7-二氢-5H-噻吩并[2,3-c]吡喃-3-羧酸酰胺或苯并[b]噻吩-3-羧酸酰胺及其药学上可接受的盐，这些衍生物用于预防和 /或治疗诸如感染性疾病，包括分泌细菌感染和机会性疾病，朊病毒疾病，免疫疾病，自身免疫疾病，双相和临床病症，心血管疾病，细胞增殖性疾病，糖尿病，炎症，移植排斥，勃起功能障碍，神经变性 疾病和中风，以及含有至少一种杂双环化合物和/或其药学上可接受的盐的组合物。 此外，公开了用于合成杂双环化合物的反应程序。

公开(公告)号：US20070191344A1

公开(公告)日：2007-08-16

申请号：US10572043

申请日：2004-09-15

申请人： Axel Choidas ,  Alexander Backes ,  Matt Cotten ,  Ola Engkvist ,  Beatrice Felber ,  Achim Freisleben ,  Klaus Godl ,  Zoltan Greff ,  Peter Habenberger ,  Doris Hafenbradl ,  Christian Hartung ,  Thomas Herget ,  Edmund Hoppe ,  Bert Klebl ,  Andrea Missio ,  Gerhard Muller ,  Wilfried Schwab ,  Birgit Zech ,  Jose Bravo ,  John Harris ,  Joelle Le ,  Jackie Macritchie ,  Vladimir Savic ,  Brad Sherborne ,  Don Simpson

发明人： Axel Choidas ,  Alexander Backes ,  Matt Cotten ,  Ola Engkvist ,  Beatrice Felber ,  Achim Freisleben ,  Klaus Godl ,  Zoltan Greff ,  Peter Habenberger ,  Doris Hafenbradl ,  Christian Hartung ,  Thomas Herget ,  Edmund Hoppe ,  Bert Klebl ,  Andrea Missio ,  Gerhard Muller ,  Wilfried Schwab ,  Birgit Zech ,  Jose Bravo ,  John Harris ,  Joelle Le ,  Jackie Macritchie ,  Vladimir Savic ,  Brad Sherborne ,  Don Simpson

IPC分类号： A61K31/55 ,  A61K31/506 ,  C07D403/02

CPC分类号： C04B35/632 ,  C07D239/42 ,  C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12

摘要： The present invention relates to 4,6-disubstituted aminopyrimidine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, and pharmaceutical compositions containing at least one of said 4,6-di substituted aminopyrimidine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said 4,6-disubstituted aminopyrimidine derivatives as inhibitors for a protein kinase and a medium comprising at least one of said 4,6-disubstituted aminopyrimidine derivatives in an immobilized form and the use of said medium for enriching, purifying and/or depleting nucleotide binding proteins which bind to the immobilized 4,6-disubstituted aminopyrimidine derivatives.

摘要翻译： 本发明涉及4,6-二取代的氨基嘧啶衍生物和/或其药学上可接受的盐，这些衍生物作为药物活性剂的用途，特别是用于预防和/或治疗感染性疾病，包括机会性疾病，朊病毒疾病，免疫学 疾病，自身免疫疾病，双相和临床疾病，心血管疾病，细胞增殖性疾病，糖尿病，炎症，移植排斥，勃起功能障碍，神经变性疾病和中风，以及含有所述4,6-二取代氨基嘧啶衍生物和 /或其药学上可接受的盐。 此外，本发明涉及所述4,6-二取代氨基嘧啶衍生物作为蛋白激酶的抑制剂和包含至少一种固定化形式的所述4,6-二取代氨基嘧啶衍生物的介质和使用所述培养基 用于富集，纯化和/或消除与固定的4,6-二取代氨基嘧啶衍生物结合的核苷酸结合蛋白。

公开(公告)号：US08084457B2

公开(公告)日：2011-12-27

申请号：US10572043

申请日：2004-09-15

申请人： Axel Choidas ,  Alexander Backes ,  Matt Cotten ,  Ola Engkvist ,  Beatrice Felber ,  Achim Freisleben ,  Klaus Godl ,  Zoltán Greff ,  Peter Habenberger ,  Doris Hafenbradl ,  Christian Hartung ,  Thomas Herget ,  Edmund Hoppe ,  Bert Klebl ,  Andrea Missio ,  Gerhard Müller ,  Wilfried Schwab ,  Birgit Zech ,  Jose Bravo ,  John Harris ,  Joelle Le ,  Jackie Macritchie ,  Vladimir Savic ,  Brad Sherborne ,  Don Simpson

发明人： Axel Choidas ,  Alexander Backes ,  Matt Cotten ,  Ola Engkvist ,  Beatrice Felber ,  Achim Freisleben ,  Klaus Godl ,  Zoltán Greff ,  Peter Habenberger ,  Doris Hafenbradl ,  Christian Hartung ,  Thomas Herget ,  Edmund Hoppe ,  Bert Klebl ,  Andrea Missio ,  Gerhard Müller ,  Wilfried Schwab ,  Birgit Zech ,  Jose Bravo ,  John Harris ,  Joelle Le ,  Jackie Macritchie ,  Vladimir Savic ,  Brad Sherborne ,  Don Simpson

IPC分类号： A01N43/54 ,  C07D239/42 ,  C07D401/04 ,  C07D239/00 ,  C07D239/02

CPC分类号： C04B35/632 ,  C07D239/42 ,  C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12

摘要： The present invention relates to 4,6-disubstituted aminopyrimidine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, and pharmaceutical compositions containing at least one of said 4,6-di substituted aminopyrimidine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said 4,6-disubstituted aminopyrimidine derivatives as inhibitors for a protein kinase and a medium comprising at least one of said 4,6-disubstituted aminopyrimidine derivatives in an immobilized form and the use of said medium for enriching, purifying and/or depleting nucleotide binding proteins which bind to the immobilized 4,6-disubstituted aminopyrimidine derivatives.

摘要翻译： 本发明涉及4,6-二取代的氨基嘧啶衍生物和/或其药学上可接受的盐，这些衍生物作为药物活性剂的用途，特别是用于预防和/或治疗感染性疾病，包括机会性疾病，朊病毒疾病，免疫学 疾病，自身免疫疾病，双相和临床疾病，心血管疾病，细胞增殖性疾病，糖尿病，炎症，移植排斥，勃起功能障碍，神经变性疾病和中风，以及含有所述4,6-二取代氨基嘧啶衍生物和 /或其药学上可接受的盐。 此外，本发明涉及所述4,6-二取代氨基嘧啶衍生物作为蛋白激酶的抑制剂和包含至少一种固定化形式的所述4,6-二取代氨基嘧啶衍生物的介质和使用所述培养基 用于富集，纯化和/或消除与固定的4,6-二取代氨基嘧啶衍生物结合的核苷酸结合蛋白。