公开(公告)号：EP1833832A1

公开(公告)日：2007-09-19

申请号：EP06847011.1

申请日：2006-01-02

申请人： GPC Biotech AG

发明人： MÜLLER, Stefan ,  SCHWAB, Wilfried ,  KLEBL, Bert ,  HAFENBRADL, Doris ,  HOPPE, Edmund ,  HORVATH, Zoltán ,  KERI, György ,  VARGA, Zoltán ,  ÖRFI, László ,  MAROSFALVI, Jenö ,  MÜLLER, Gerhard

IPC分类号： C07D471/04 ,  A61K31/4375 ,  A61P7/02 ,  A61P9/00 ,  A61P11/06 ,  A61P19/10 ,  A61P15/10 ,  A61P27/06 ,  A61P29/00 ,  A61P31/00 ,  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.

公开(公告)号：EP1670804A2

公开(公告)日：2006-06-21

申请号：EP04786934.2

申请日：2004-09-10

申请人： GPC Biotech AG

发明人： KOUL, Anil ,  KLEBL, Bert ,  MÜLLER, Gerhard ,  MISSIO, Andrea ,  SCHWAB, Wilfried ,  HAFENBRADL, Doris ,  NEUMANN, Lars ,  SOMMER, Marc-Nicola ,  MÜLLER, Stefan ,  HOPPE, Edmund ,  FREISLEBEN, Achim ,  BACKES, Alexander ,  HARTUNG, Christian ,  FELBER, Beatrice ,  ZECH, Birgit ,  ENGKVIST, Ola ,  KERI, György ,  ÖRFI, Laszlo ,  BANHEGYI, Peter ,  GREFF, Zoltan ,  HORVATH, Zoltan ,  VARGA, Zoltan ,  MARKO, Péter ,  PATO, Jànos ,  SZABADKAI, Istvan ,  SZEKELYHIDI, Zsolt ,  WACZEK, Frigyes

IPC分类号： C07D495/04 ,  C07D495/10 ,  C07D493/04 ,  C07D491/04 ,  C07D409/12 ,  C07D333/66 ,  C07D333/68 ,  C07D209/42 ,  A61K31/381 ,  A61P31/04

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.

公开(公告)号：EP1786781A2

公开(公告)日：2007-05-23

申请号：EP05785583.5

申请日：2005-08-29

申请人： GPC Biotech AG

发明人： KLEBL, Bert ,  BAUMANN, Matthias ,  HOPPE, Edmund ,  BREHMER, Dirk ,  DAUB, Henrik ,  KERI, György ,  VARGA, Zoltán ,  MAROSFALVI, Jenö ,  ÖRFI, Lászl

IPC分类号： C07D239/42

CPC分类号： C07D239/42 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14

摘要： The present invention relates to pyrimidine derivatives, methods for their synthesis, and the use of said pyrimidine derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of cell proliferation disorders, cancer, leukemia, erectile dysfunction, cardiovascular diseases and disorders, inflammatory diseases, transplant rejection, immunological diseases, neuroimmunological diseases, autoimmune diseases, infective diseases including opportunistic infections, prion diseases and/or neuro-degeneration. Furthermore, the present invention relates to pharmaceutical compositions containing at least one pyrimidine derivative and/or pharmaceutically acceptable salts thereof as an active ingredient together with at least one pharmaceutically acceptable carrier, excipient or diluents as well as to methods for prophylaxis and/or treatment of the above-mentioned diseases and disorders.

公开(公告)号：EP1678147A1

公开(公告)日：2006-07-12

申请号：EP04786953.2

申请日：2004-09-15

申请人： GPC Biotech AG

发明人： CHOIDAS, Axel ,  BACKES, Alexander ,  COTTEN, Matt ,  ENGKVIST, Ola ,  FELBER, Beatrice ,  FREISLEBEN, Achim ,  GODL, Klaus ,  GREFF, Zoltán ,  HABENBERGER, Peter ,  HAFENBRADL, Doris ,  HARTUNG, Christian ,  HERGET, Thomas ,  HOPPE, Edmund ,  KLEBL, Bert ,  MISSIO, Andrea ,  MÜLLER, Gerhard ,  SCHWAB, Wilfried ,  ZECH, Birgit ,  BRAVO, Jose ,  HARRIS, John ,  LE, Joelle ,  MACRITCHIE, Jackie ,  SAVIC, Vladimir ,  SHERBORNE, Brad ,  SIMPSON, Don

IPC分类号： C07D239/42 ,  C07D401/12 ,  C07D239/48 ,  C07D403/12 ,  C07D401/04 ,  C07D409/12 ,  C07D417/12 ,  C07D405/12 ,  C07D409/14 ,  C07D413/12 ,  C07D409/04 ,  A61K31/505

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. Furhtermore, 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.