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1.发明公开
公开(公告)号：EP3684762A1
公开(公告)日：2020-07-29
申请号：EP18769382.5
申请日：2018-09-20
申请人： Lead Discovery Center GmbH , Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. , Sotio a.s.
发明人： DI LUCREZIA, Raffaella , BERGBREDE, Tim , NUSSBAUMER, Peter , KOCH, Uwe , KLEBL, Bert , CHOIDAS, Axel , UNGER, Anke , LARSSON, Nils-Göran , FALKENBERG-GUSTAFSSON, Maria , GUSTAFSSON, Claes M.
IPC分类号： C07D311/18 , C07D405/12 , A61K31/37 , A61P35/00
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公开(公告)号：EP2748331A1
公开(公告)日：2014-07-02
申请号：EP12761556.5
申请日：2012-08-22
发明人： CHOIDAS, Axel , KLEBL, Bert , HABENBERGER, Peter , EICKHOFF, Jan , THOMAS, Roman , HEUCKMANN, Johannes
IPC分类号： C12Q1/68
CPC分类号： G01N33/5011 , C12Q1/6881 , C12Q1/6886 , C12Q2600/106 , G01N2800/52
摘要： The present invention relates to a method of selecting (a) cell(s), (a) tissue(s) or (a) cell culture(s) with susceptibility to a selective CDK9 inhibitor. Also a method for determining the responsiveness of a mammalian tumor cell or cancer cell to treatment with a selective CDK9 inhibitor is described herein. In particular, the present invention provides for an in vitro method for the identification of a responder for or a patient sensitive to a selective CDK9 inhibitor, whereby the patient is suspected to suffer from NUT midline carcinoma (NMC). The present invention also relates to a method of monitoring or predicting the efficacy of a treatment of NUT midline carcinoma (NMC), wherein treatment with a selective CDK9 inhibitor is in particular envisaged. Also the use of a (transgenic) non-human animal or a (transgenic) cell having at least one rearrangement in the NUT gene for screening and/or validation of a medicament for the treatment NUT midline carcinoma (NMC) is described. Furthermore, a kit useful for carrying out the methods described herein as well as an olieo- or polynucleotide canable of detecting rearrangements in the NUT nene are provided.
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公开(公告)号：EP2747755A1
公开(公告)日：2014-07-02
申请号：EP12761554.0
申请日：2012-08-22
发明人： CHOIDAS, Axel , KLEBL, Bert , HABENBERGER, Peter , EICKHOFF, Jan , THOMAS, Roman , HEUCKMANN, Johannes
IPC分类号： A61K31/00 , A61K31/4418 , A61K31/53 , A61P35/00
CPC分类号： C07C53/18 , A61K31/4418 , A61K31/53 , C07D213/40 , C07D213/74 , C07D251/16 , C07D251/22 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/10 , C07D471/04
摘要： The present invention relates to a CDK9 inhibitor, especially a selective CDK9 inhibitor, for use in treating, ameliorating and/or preventing midline carcinoma. Also corresponding methods for treating, preventing or ameliorating midline carcinoma are subject of the present invention. Preferably, NUT midline carcinoma is treated with the CDK9 inhibitors in accordance with the present invention.
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公开(公告)号：EP2609091B1
公开(公告)日：2014-11-26
申请号：EP11754617.6
申请日：2011-08-26
发明人： SCHULTZ-FADEMRECHT, Carsten , KLEBL, Bert , CHOIDAS, Axel , KOCH, Uwe , EICKHOFF, Jan , WOLF, Alexander , ULLRICH, Axel
IPC分类号： C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D215/233 , A61K31/4709 , A61P35/00
CPC分类号： C07D401/12 , A61K31/47 , A61K31/495 , C07D215/233 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
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公开(公告)号：EP2609091A1
公开(公告)日：2013-07-03
申请号：EP11754617.6
申请日：2011-08-26
发明人： SCHULTZ-FADEMRECHT, Carsten , KLEBL, Bert , CHOIDAS, Axel , KOCH, Uwe , EICKHOFF, Jan , WOLF, Alexander , ULLRICH, Axel
IPC分类号： C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , A61K31/4709 , A61P35/00
CPC分类号： C07D401/12 , A61K31/47 , A61K31/495 , C07D215/233 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention relates to 1-nitrogen-heterocyclic-2-carboxamides of general formula (I): and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the treatment and/or prevention of Axl receptor tyrosine kinase subfamily induced disorders, including cancer and primary tumor metastases, and pharmaceutical compositions containing at least one of said 1-nitrogen-heterocyclic-2-carboxamide derivatives and/or pharmaceutically acceptable salts thereof.
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公开(公告)号：EP4333822A1
公开(公告)日：2024-03-13
申请号：EP22727767.0
申请日：2022-05-02
发明人： BERGBREDE, Tim , UNGER, Anke , DI LUCREZIA, Raffaella , CHOIDAS, Axel , KLEBL, Bert , NUSSBAUMER, Peter , MENNINGER, Sascha , HABENBERGER, Peter , ZISCHINSKY, Gunther , KOCH, Uwe , SCHRÖDER, Peter , JESTRABOVÁ, Pavla , PALOVÁ-JELÍNKOVÁ, Lenka , DÁNOVÁ, Klára , FALKENBERG-GUSTAFSSON, Maria , ARABANIAN, Laleh , GUSTAFSSON, Claes , LARSSON, Nils-Göran , PALMQVIST, Lars
IPC分类号： A61K31/166 , A61K31/167 , A61K31/4184 , A61K31/437 , A61K31/4412 , A61K31/4439 , A61K31/4523 , A61K31/453 , A61K31/4709 , A61K31/496 , A61K31/502 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/5517 , A61P35/00
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公开(公告)号：EP2748331B1
公开(公告)日：2016-03-02
申请号：EP12761556.5
申请日：2012-08-22
发明人： CHOIDAS, Axel , KLEBL, Bert , HABENBERGER, Peter , EICKHOFF, Jan , THOMAS, Roman , HEUCKMANN, Johannes
IPC分类号： C12Q1/68
CPC分类号： G01N33/5011 , C12Q1/6881 , C12Q1/6886 , C12Q2600/106 , G01N2800/52
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公开(公告)号：EP3613738A1
公开(公告)日：2020-02-26
申请号：EP18190603.3
申请日：2018-08-23
发明人： SCHULTZ-FADEMRECHT, Carsten , KLEBL, Bert , NUSSBAUMER, Peter , DEGENHART, Carsten , BAUMANN, Matthias
IPC分类号： C07D471/04
摘要： The present invention relates to certain 4-substituted 1 H -pyrrolo[2,3-b]pyridine compounds of the formula (I) and pharmaceutically acceptable salts thereof. These compounds is useful in the treatment or prevention of a disease or medical condition mediated through certain mutated forms of ErbB receptor, especially of Exon20 Her2 and EGFR mutations.
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公开(公告)号：EP4301736A1
公开(公告)日：2024-01-10
申请号：EP22797303.9
申请日：2022-09-25
发明人： KOCH, Uwe , ZISCHINSKY, Gunther , UNGER, Anke , NUSSBAUMER, Peter , KLEBL, Bert , CHOIDAS, Axel , DINKEL, Klaus , ENGEL, Julian , DEGENHART, Carsten , HUBER, Robert , NAM, Kiyean , KIM, Jaeseung , SEO, Jeongjea , LEE, Seung-Joo , JEON, Yeejin , AHN, Wongyun
IPC分类号： C07D273/00 , A61P35/00 , A61K31/33 , C07D491/08
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10.发明授权PHARMACEUTICALLY ACTIVE 4,6-DISUBSTITUTED AMINOPYRIMIDINE DERIVATIVES AS MODULATORS OF PROTEIN KINASES 有权药学有效4,6-二取代氨基嘧啶衍生物作为蛋白激酶的调节剂
公开(公告)号：EP1678147B1
公开(公告)日：2012-08-08
申请号：EP04786953.2
申请日：2004-09-15
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.
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