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公开(公告)号:US20240415819A1
公开(公告)日:2024-12-19
申请号:US18694432
申请日:2022-09-25
Applicant: Lead Discovery Center GmbH , QLI5 THERAPEUTICS AG
Inventor: Uwe Koch , Gunther Zischinsky , Anke Unger , Peter Nussbaumer , Bert Klebl , Axel Choidas , Klaus Dinkel , Julian Engel , Carsten Degenhart , Robert Huber , Kiyean Nam , Jaesung Kim , Jeongjea Seo , Seung-Joo Lee , Yeejin Jeon , Wongyun Ahn
IPC: A61K31/439 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/5386 , A61P35/00 , C07D498/08 , C07D519/00
Abstract: The present invention relates to certain macrocyclic compounds of the formula (I) and pharmaceutically acceptable salts thereof. These compounds are useful in the treatment or prevention of a disease associated with and/or caused by proteasome or immunoproteasome, selected from a cancer, an infectious disease, an inflammatory disease, and autoimmune disease.
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公开(公告)号:US12060362B2
公开(公告)日:2024-08-13
申请号:US17273549
申请日:2019-09-05
Applicant: LEAD DISCOVERY CENTER GMBH , MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WISSENSCHAFTEN E.V.
Inventor: Herbert Waldmann , Gunther Zischinsky , Peter Nussbaumer , Slava Ziegler , Melanie Schwalfenberg , Javier de Ceballos Cerrajeria , Elena Sabrina Reckzeh , George Karageorgis
IPC: C07D491/08 , A61K31/529
CPC classification number: C07D491/08
Abstract: The present invention relates to 2,6-methanobenzo[g][1]oxacin-4-one compounds and their analog compounds and pharmaceutically acceptable salts thereof as selective inhibitor of glucose transporters 1 and 3 (GLUTs 1 and 3), to methods of preparing said compounds, and to the use thereof as pharmaceutically active agents, especially for the prophylaxis and/or treatment of metabolic diseases, immunological diseases, autoimmune diseases, inflammation, graft versus host disease, cancer, and metastasis thereof. Furthermore, the present invention is directed to pharmaceutical composition comprising at least one of 2,6-methanobenzo[g][1]oxacin-4-one compounds and their analog compounds.
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3.
公开(公告)号:US20220169616A1
公开(公告)日:2022-06-02
申请号:US17440468
申请日:2020-03-19
Applicant: Lead Discovery Center GmbH
Inventor: Raffaella Di Lucrezia , Tim Bergbrede , Peter Nussbaumer , Peter Schröder
IPC: C07D215/20 , A61K31/47 , C07D401/12 , A61K31/4709 , A61K31/4375 , C07D471/04 , C07D471/10 , A61K31/438 , A61K45/06 , A61P35/00 , C07D491/107 , A61K31/5377 , C07D519/00
Abstract: The present invention relates to compounds of the general formula (I): (I), wherein V, W, M, R, R and Y have the designations cited below, or a pharmaceutically or veterinary acceptable salt, hydrate or solvate thereof, and to processes for the preparation of compounds of the general formula (I) or a pharmaceutically or veterinary acceptable salt, hydrate or solvate thereof. The invention also relates to compounds of the general formula (I) or a pharmaceutically or veterinary acceptable salt, hydrate or solvate thereof for use as a medicament. Further, the invention relates to compounds of the general formula (I) or a pharmaceutically or veterinary acceptable salt, hydrate or solvate thereof for use in the treatment of cancer. Moreover, the invention relates to compounds of the general formula (I) or a pharmaceutically or veterinary acceptable salt, hydrate or solvate thereof for treating cancer in simultaneous, alternating or subsequent combination with another cancer therapy.
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公开(公告)号:US20220098208A1
公开(公告)日:2022-03-31
申请号:US17548978
申请日:2021-12-13
Applicant: QURIENT CO., LTD. , LEAD DISCOVERY CENTER GMBH
Inventor: KIYEAN NAM , JAESEUNG KIM , YEEJIN JEON , DONGHOON YU , MOOYOUNG SEO , DONGSIK PARK , JAN EICKHOFF , GUNTHER ZISCHINSKY , UWE KOCH
IPC: C07D487/04 , C07D519/00
Abstract: The present invention relates to pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of cell proliferative diseases, inflammatory diseases, immunological diseases, cardiovascular diseases and infectious diseases. Furthermore, the present invention is directed towards pharmaceutical compositions containing at least one of the pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives and/or pharmaceutically acceptable salts thereof.
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5.
公开(公告)号:US20200291011A1
公开(公告)日:2020-09-17
申请号:US16648348
申请日:2018-09-20
Applicant: Lead Discovery Center GmbH , Max Planck Gesellschaft zur Förderung der Wissenschften e.V. , SOTIO a.s.
Inventor: Raffaella Di Lucrezia , Tim Bergbrede , Peter Nussbaumer , Uwe Koch , Bert Klebl , Axel Choidas , Anke Unger , Nils-Göran Larsson , Maria Falkenberg-Gustafsson , Claes M. Gustafsson
IPC: C07D413/14 , C07D405/12 , C07D311/18 , C07D491/052 , C07D409/14 , C07D409/04
Abstract: The invention provides novel coumarin derivatives as specific mitochondrial RNA polymerase inhibitors for the treatment of cancer.
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6.
公开(公告)号:US20200031794A1
公开(公告)日:2020-01-30
申请号:US16519856
申请日:2019-07-23
Applicant: Lead Discovery Center GmbH , Max Planck Gesellschaft zur Förderung der Wissenschaften e. V.
Inventor: Raffaella Di Lucrezia , Tim Bergbrede , Peter Nussbaumer , Uwe Koch , Bert Klebl , Axel Choidas , Anke Unger , Nils-Göran Larsson , Maria Falkenberg-Gustafsson , Claes M. Gustafsson
IPC: C07D311/54 , C07D407/12 , C07D407/14 , C07D413/12
Abstract: The invention provides novel 4-phenyl-coumarin derivatives, processes for their preparation and uses thereof as specific mitochondrial RNA polymerase inhibitors for the treatment of cancer.
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公开(公告)号:US20240252454A1
公开(公告)日:2024-08-01
申请号:US18289283
申请日:2022-05-02
Applicant: LEAD DISCOVERY CENTER GMBH , MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WISSENSCHAFTEN E.V.
Inventor: Tim BERGBREDE , Raffaella DI LUCREZIA , Anke UNGER , Axel CHOIDAS , Bert KLEBL , Peter NUSSBAUMER , Sascha MENNINGER , Peter HABENBERGER , Gunther ZISCHINSKY , Uwe KOCH , Peter SCHRÖDER , Pavla JESTRABOVÁ , Lenka PALOVÁ-JELÍNKOVÁ , Klára DÁNOVÁ , Maria FALKENBERG-GUSTAFSSON , Laleh ARABANIAN , Claes GUSTAFSSON , Nils-Göran LARSSON , Lars PALMQVIST
IPC: A61K31/166 , A61K31/4184 , A61K31/453 , A61K31/47 , A61K31/496 , A61K31/5377 , A61K31/711 , A61P35/00
CPC classification number: A61K31/166 , A61K31/4184 , A61K31/453 , A61K31/47 , A61K31/496 , A61K31/5377 , A61K31/711 , A61P35/00
Abstract: The present invention relates to a composition comprising at least one inhibitor of mitochondrial transcription (IMT) and at least one anti-cancer drug. Furthermore, the present invention is directed to compositions for use as a medicament and to compositions for use in the treatment and/or prevention of cancer.
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8.
公开(公告)号:US11858937B2
公开(公告)日:2024-01-02
申请号:US17045009
申请日:2019-04-11
Applicant: QURIENT CO., LTD. , LEAD DISCOVERY CENTER GMBH
Inventor: Kiyean Nam , Jaeseung Kim , Yeejin Jeon , Donghoon Yu , Mooyoung Seo , Dongsik Park , Jan Eickhoff , Gunther Zischinsky , Uwe Koch
IPC: A61K31/519 , A61K31/53 , C07D487/04
CPC classification number: C07D487/04
Abstract: The present invention relates to pyrazolo [1,5-a][1,3,5]triazine and pyrazolo [1,5-a]pyrimidine derivatives having Formula I:
and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of cell proliferative diseases, inflammatory diseases, immunological diseases, cardiovascular diseases and infectious diseases. Furthermore, the present invention is directed towards pharmaceutical compositions containing at least one of the pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives and/or pharmaceutically acceptable salts thereof.-
公开(公告)号:US20220370440A1
公开(公告)日:2022-11-24
申请号:US17270221
申请日:2019-08-23
Applicant: Lead Discovery Center GmbH
Inventor: Carsten Schultz-Fademrecht , Bert Klebl , Peter Nussbaumer , Carsten Degenhart , Matthias Baumann
IPC: A61K31/496 , A61K45/06 , C07D471/04 , A61K31/4545 , A61K31/437 , A61K31/5377 , A61K31/506 , A61K31/538 , A61K31/4709
Abstract: The present invention relates to certain 4-substituted 1H-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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10.
公开(公告)号:US11111238B2
公开(公告)日:2021-09-07
申请号:US16648348
申请日:2018-09-20
Applicant: Lead Discovery Center GmbH , Max Planck Gesellschaft zur Förderung der Wissenschaften e. V. , SOTIO a.s.
Inventor: Raffaella Di Lucrezia , Tim Bergbrede , Peter Nussbaumer , Uwe Koch , Bert Klebl , Axel Choidas , Anke Unger , Nils-Göran Larsson , Maria Falkenberg-Gustafsson , Claes M. Gustafsson
IPC: A61K45/06 , C07D413/14 , C07D311/18 , C07D405/12 , C07D409/04 , C07D409/14 , C07D491/052
Abstract: The invention provides novel coumarin derivatives as specific mitochondrial RNA polymerase inhibitors for the treatment of cancer.
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