公开(公告)号：US20080207677A1

公开(公告)日：2008-08-28

申请号：US11813236

申请日：2006-01-02

申请人： Stefan Muller ,  Wilfried Schwab ,  Bert Klebl ,  Doris Hafenbradl ,  Edmund Hoppe ,  Zoltan Horvath ,  Gyorgy Keri ,  Zoltan Varga ,  Laszlo Orfi ,  Jeno Marosfalvi ,  Gerhard Muller

发明人： Stefan Muller ,  Wilfried Schwab ,  Bert Klebl ,  Doris Hafenbradl ,  Edmund Hoppe ,  Zoltan Horvath ,  Gyorgy Keri ,  Zoltan Varga ,  Laszlo Orfi ,  Jeno Marosfalvi ,  Gerhard Muller

IPC分类号： A61K31/4375 ,  C07D471/04 ,  A61P35/00

CPC分类号： C07D471/04

摘要： The present invention relates to compounds having a naphthyridine scaffold, and stereoisomeric forms, prodrugs, solvates, hydrates and/or pharmaceutically acceptable salts of these compounds as well as pharmaceutical compositions containing at least one of these naphthyridine derivatives together with pharmaceutically acceptable carrier, excipient and/or diluents. Said naphthyridine compounds have been identified as inhibitors of the protein kinase ROCK2, also known as Rho-kinase, and are useful for the treatment of cancers (tumor growth and metastases), erectile dysfunction, cardiovascular diseases, hypertension, angina pectoris, cerebral ischaemia, cerebral vasospasm, myocardial ischaemia, coronary vasospasm, heart failure, myocardial hypertrophy, atherosclerosis, restenosis, spinal cord injuries, neuronal degeneration, thrombotic disorders, asthma, glaucoma, inflammation, anti-viral diseases (e.g. HIV), and osteoporosis.

摘要翻译： 本发明涉及具有萘啶支架的化合物，以及这些化合物的立体异构形式，前体药物，溶剂合物，水合物和/或药学上可接受的盐，以及含有这些萘啶衍生物中至少一种以及药学上可接受的载体，赋形剂和 /或稀释剂。 所述萘啶化合物已被鉴定为蛋白激酶ROCK2（也称为Rho-激酶）的抑制剂，可用于治疗癌症（肿瘤生长和转移），勃起功能障碍，心血管疾病，高血压，心绞痛，脑缺血， 脑血管痉挛，心肌缺血，冠状动脉血管痉挛，心力衰竭，心肌肥大，动脉粥样硬化，再狭窄，脊髓损伤，神经元变性，血栓形成障碍，哮喘，青光眼，炎症，抗病毒疾病（例如HIV）和骨质疏松症。

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。

公开(公告)号：US20090196912A1

公开(公告)日：2009-08-06

申请号：US11659013

申请日：2005-08-01

申请人： Jan Elke Eickhoff ,  Doris Hafenbradl ,  Wilfried Schwab ,  Matthew Cotton ,  Bert Matthias Kiebl ,  Birgit Zech ,  Stefan Muller ,  John Harris ,  Vladimir Savic ,  Jackie MacRitchie

发明人： Jan Elke Eickhoff ,  Doris Hafenbradl ,  Wilfried Schwab ,  Matthew Cotton ,  Bert Matthias Kiebl ,  Birgit Zech ,  Stefan Muller ,  John Harris ,  Vladimir Savic ,  Jackie MacRitchie

IPC分类号： A61K9/127 ,  C07D213/72 ,  A61K31/44 ,  C07D401/04 ,  A61K31/506 ,  A61K31/443 ,  C07D405/12 ,  C07D413/02 ,  A61K31/5377 ,  A61K9/28 ,  A61P35/00 ,  A61P3/10

CPC分类号： C07D213/74

摘要： Described are pyridinylamines and pharmaceutically acceptable salts thereof, the use of these pyridinylamines for the prophylaxis and/or treatment of various diseases such as infectious diseases, including opportunistic infections, 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 pharmaceutical compositions containing at least one pyridinylamine and/or pharmaceutically acceptable salts thereof. Furthermore, reaction procedures for the synthesis of the pyridinylamines are disclosed.

摘要翻译： 描述的是吡啶基胺及其药学上可接受的盐，这些吡啶基胺用于预防和/或治疗各种疾病如传染病，包括机会性感染，朊病毒免疫疾病，自身免疫性疾病，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，以及含有至少一种吡啶胺和/或其药学上可接受的盐的药物组合物。 此外，公开了吡啶基胺的合成反应程序。

公开(公告)号：US20080194574A1

公开(公告)日：2008-08-14

申请号：US10596508

申请日：2004-12-16

申请人： Jan Eike Eikhoff ,  Mark Richard Ashton ,  Stephen Martin Courtney ,  Christopher John Yarnold ,  Maurizio Varrone ,  Pui Leng Loke ,  Thomas Herget ,  Wilfried Schwab ,  Doris Hafenbradl

发明人： Jan Eike Eikhoff ,  Mark Richard Ashton ,  Stephen Martin Courtney ,  Christopher John Yarnold ,  Maurizio Varrone ,  Pui Leng Loke ,  Thomas Herget ,  Wilfried Schwab ,  Doris Hafenbradl

IPC分类号： A61K31/4985 ,  C07D487/04 ,  C07D241/10 ,  A61K31/4965 ,  A61P31/00 ,  A61P37/00 ,  A61P25/16 ,  A61P25/28

CPC分类号： C07D401/04 ,  C07D241/20 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14

摘要： The present invention relates to pyrazine derivatives according to the general formula (I) and pharmaceutically acceptable salts thereof and their use as pharmaceutical compounds as well as the use of these compounds for the preparation of a pharmaceutical composition 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, stroke and especially for the treatment of herpesviral induced infections, including opportunistic infections as well as infections and diseases caused by human cytomegalovirus (HCMV).

摘要翻译： 本发明涉及根据通式（I）的吡嗪衍生物及其药学上可接受的盐及其作为药物化合物的用途，以及这些化合物在制备用于预防和/或治疗感染性疾病的药物组合物中的用途 疾病，包括机会性疾病，朊病毒疾病，免疫疾病，自身免疫性疾病，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，中风，特别是治疗疱疹病毒诱导的感染 ，包括机会性感染以及由巨细胞病毒（HCMV）引起的感染和疾病。

公开(公告)号：US08507498B2

公开(公告)日：2013-08-13

申请号：US12451039

申请日：2008-04-24

申请人： Philipp Wabnitz ,  Heike Schauerte ,  Hans Allgeier ,  Martin Augustin ,  Lutz Zeitlmann ,  Michael A. Pleiss ,  Gabriele Stumm ,  Anke Mueller ,  Axel Choidas ,  Bert Klebl ,  Gerhard Mueller ,  Wilfried Schwab ,  Joelle Le ,  Jackie Macritchie ,  Don Simpson

发明人： Philipp Wabnitz ,  Heike Schauerte ,  Hans Allgeier ,  Martin Augustin ,  Lutz Zeitlmann ,  Michael A. Pleiss ,  Gabriele Stumm ,  Anke Mueller ,  Axel Choidas ,  Bert Klebl ,  Gerhard Mueller ,  Wilfried Schwab ,  Joelle Le ,  Jackie Macritchie ,  Don Simpson

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

CPC分类号： C07D239/42 ,  C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

摘要： The present invention relates to inhibitors of general Formula (I) of cyclin-dependent kinases and therapeutic applications thereof. Furthermore, the invention relates to compounds for preventing and/or treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases.

摘要翻译： 本发明涉及细胞周期蛋白依赖性激酶的通式（I）的抑制剂及其治疗应用。 此外，本发明涉及用于预防和/或治疗任何类型的疼痛，炎症性疾病，免疫疾病，增殖性疾病，感染性疾病，心血管疾病和神经变性疾病的化合物。

公开(公告)号：US20110306602A1

公开(公告)日：2011-12-15

申请号：US12451039

申请日：2008-04-24

申请人： Philipp Wabnitz ,  Heike Schauerte ,  Hans Allgeier ,  Lutz Zeitlmann ,  Anke Mueller ,  Martin Augustin ,  Michael A. Pleiss ,  Gabriele Stumm ,  Axel Choidas ,  Bert Klebl ,  Gerhard Mueller ,  Wilfried Schwab ,  Joelle Le ,  Jackie Macritchie ,  Don Simpson

发明人： Philipp Wabnitz ,  Heike Schauerte ,  Hans Allgeier ,  Lutz Zeitlmann ,  Anke Mueller ,  Martin Augustin ,  Michael A. Pleiss ,  Gabriele Stumm ,  Axel Choidas ,  Bert Klebl ,  Gerhard Mueller ,  Wilfried Schwab ,  Joelle Le ,  Jackie Macritchie ,  Don Simpson

IPC分类号： A61K31/55 ,  C07D405/12 ,  C07D409/12 ,  C07D401/12 ,  C07D413/12 ,  C07D403/12 ,  C07D417/12 ,  C07D401/10 ,  C07D413/10 ,  C07D403/10 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/506 ,  A61P29/00 ,  A61P37/00 ,  A61P35/00 ,  A61P31/00 ,  A61P9/00 ,  A61P25/28 ,  C07D239/42

CPC分类号： C07D239/42 ,  C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

摘要： The present invention relates to inhibitors of general Formula (I) of cyclin-dependent kinases and therapeutic applications thereof. Furthermore, the invention relates to compounds for preventing and/or treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases.

摘要翻译： 本发明涉及细胞周期蛋白依赖性激酶的通式（I）的抑制剂及其治疗应用。 此外，本发明涉及用于预防和/或治疗任何类型的疼痛，炎症性疾病，免疫疾病，增殖性疾病，感染性疾病，心血管疾病和神经变性疾病的化合物。

公开(公告)号：US06815440B2

公开(公告)日：2004-11-09

申请号：US10376287

申请日：2003-03-03

申请人： Werner Thorwart ,  Wilfried Schwab ,  Manfred Schudok ,  Burkhard Haase ,  Eckart Bartnik ,  Klaus-Ulrich Weithmann

发明人： Werner Thorwart ,  Wilfried Schwab ,  Manfred Schudok ,  Burkhard Haase ,  Eckart Bartnik ,  Klaus-Ulrich Weithmann

IPC分类号： C07D40102

CPC分类号： C07D405/12 ,  C07D209/42 ,  C07D217/26 ,  C07D471/04 ,  C07D491/04

摘要： Cyclic and heterocyclic N-substituted &agr;-iminohydroxamic and -carboxylic acids Compounds of the formula I are suitable for preparing pharmaceuticals for the treatment of disorders in the course of which is involved an increased activity of matrix-degrading metalloproteinases.

摘要翻译： 环状和杂环N-取代的α-亚氨基肟酸和羧酸式I的化合物适用于制备用于治疗疾病的药物，其中涉及基质降解金属蛋白酶的活性增加。

公开(公告)号：US06387934B1

公开(公告)日：2002-05-14

申请号：US09694036

申请日：2000-10-23

申请人： Wilfried Schwab ,  Ruth Raiss

发明人： Wilfried Schwab ,  Ruth Raiss

IPC分类号： A61K31435

CPC分类号： C07D333/26 ,  C07B2200/07 ,  C07C255/23 ,  C07C255/41 ,  C07C255/57 ,  C07C2601/02 ,  C07D213/57 ,  C07D307/54 ,  C07D317/60 ,  C07D333/24 ,  C07D473/04

摘要： 2-Cyano-3,5-dihydroxyhex-2-enecarboxamide derivatives are suitable for the production of pharmaceuticals for the prophylaxis and therapy of diseases or disorders whose course involves increased connective tissue or cartilage degradation.

摘要翻译： 2-氰基-3,5-二羟基己-2-烯甲酰胺衍生物适用于制备用于预防和治疗疾病或病症的药物，其病程包括增加结缔组织或软骨降解。