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1. 发明申请

WO2015136073A1 MACROCYCLIC TGF-BR2 KINASE INHIBITORS 审中-公开
标题翻译： MACROCYCLIC TGF-BR2激酶抑制剂
公开(公告)号：WO2015136073A1
公开(公告)日：2015-09-17
申请号：PCT/EP2015/055294
申请日：2015-03-13
申请人： ONCODESIGN SA
发明人： HOFLACK, Jan Marie Cyriel Jozef , BERTHET, Cyril , BENDERITTER, Pascal André René , BLOM, Petra Marcella Françoise , GOMEZ, Sylvie , DAOUBI, Mourad
IPC分类号： A61K31/519 , A61P19/04
CPC分类号： A61K31/519
摘要： The present invention relates to macrocyclic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of Transforming Growth Factor beta Receptor 2 (TGF-β R2) and/or mutants thereof, for use in the diagnosis, prevention and/or treatment of TGF-β R2 -kinase associated diseases. Moreover, the present invention provides methods of using said compounds, for instance as a medicine or diagnostic agent.
摘要翻译：本发明涉及大环化合物和含有作为激酶抑制剂的化合物的组合物，特别是作为转化生长因子β受体2（TGF-βR2）和/或其突变体的抑制剂，用于诊断，预防和/或治疗TGF-β2-2激酶相关疾病。此外，本发明提供使用所述化合物的方法，例如作为药物或诊断剂。

2. 发明申请

US20230126352A1 MACROCYCLIC RIP2-KINASE INHIBITORS 有权
公开(公告)号：US20230126352A1
公开(公告)日：2023-04-27
申请号：US17759644
申请日：2021-02-01
申请人： Oncodesign SA
发明人： Yann LAMOTTE , Nérina DODIC , Aurélien TAP , Alexis DENIS , Jean-Marie BRUSO , Mourad DAOUBI KHAMLICHI , Pascal André Rene PENDERITTER
IPC分类号： C07D498/22 , C07F7/08
摘要： The present invention relates to macrocyclic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of RIP2-kinase, and/or mutants thereof, for use in the diagnosis, prevention and/or treatment of RIP2-kinase associated diseases. Moreover, the present invention provides methods of using said compounds, for instance as a medicine or diagnostic agent.

3. 发明授权

US10716869B2 Radiolabeled macrocyclic EGFR inhibitor 有权
公开(公告)号：US10716869B2
公开(公告)日：2020-07-21
申请号：US16080196
申请日：2017-02-28
申请人： Oncodesign SA
发明人： Jan Marie Cyriel Jozef Hoflack , Cyril Berthet , Petra Marcella Françoise Blom , Johnny Vercouillie , Caroline Robic , Sarah Catoen , Gilles Voit , Jean-Bernard Deloye
IPC分类号： A61K51/00 , A61M36/14 , A61K51/04 , C07D498/08 , C07B59/00 , A61B6/03 , A61P35/00
摘要： The present invention relates to 18-Fluor radiolabeled macrocyclic quinazoline compounds, which are suitable as positron emission tomography (PET) tracers for imaging epidermal growth factor receptors (EGFR), and their use in in vivo diagnosis, preclinical and clinical tumour imaging, patient stratification on the basis of mutational status of EGFR, and assessing tumour response to therapeutic treatments. The present invention also describes precursor compounds and methods of preparing the radiotracers. The invention is relevant to any cancer that is influenced or driven by deregulated EGFR, such as, but not limited to, non-small cell lung cancer (NSCLC), pancreatic, hepatocellular, oesophageal, gastric, colorectal, prostate, cervical, renal, ovarian, breast cancers, head and neck squamous cell carcinoma, and malignant glioma.

4. 发明申请

US20190054197A1 RADIOLABELED MACROCYCLIC EGFR INHIBITOR 审中-公开
公开(公告)号：US20190054197A1
公开(公告)日：2019-02-21
申请号：US16080196
申请日：2017-02-28
申请人： Oncodesign SA
发明人： Jan Marie Cyriel Jozef Hoflack , Cyril Berthet , Petra Marcella Françoise Blom , Johnny Vercouillie , Caroline Robic , Sarah Catoen
IPC分类号： A61K51/04 , A61B6/03
摘要： The present invention relates to 18-Fluor radiolabeled macrocyclic quinazoline compounds, which are suitable as positron emission tomography (PET) tracers for imaging epidermal growth factor receptors (EGFR), and their use in in vivo diagnosis, preclinical and clinical tumour imaging, patient stratification on the basis of mutational status of EGFR, and assessing tumour response to therapeutic treatments. The present invention also describes precursor compounds and methods of preparing the radiotracers. The invention is relevant to any cancer that is influenced or driven by deregulated EGFR, such as, but not limited to, non-small cell lung cancer (NSCLC), pancreatic, hepatocellular, oesophageal, gastric, colorectal, prostate, cervical, renal, ovarian, breast cancers, head and neck squamous cell carcinoma, and malignant glioma.

5. 发明申请

WO2021224320A1 NEW MACROCYCLIC LRRK2 KINASE INHIBITORS 审中-公开
公开(公告)号：WO2021224320A1
公开(公告)日：2021-11-11
申请号：PCT/EP2021/061827
申请日：2021-05-05
申请人： LES LABORATOIRES SERVIER , ONCODESIGN SA
发明人： BLOM, Petra Marcella , HOUSSEMAN, Christopher Gaétan , DAUGAN, Alain , DUMOULIN, Audrey , LAUGEOIS, Maxime , DENIS, Alexis , FAUCHER, Nicolas , BOTEZ, Iuliana , LE TIRAN, Arnaud , CHRISTENSEN, Kenneth , LAMOTTE, Yann
IPC分类号： C07D498/16 , C07D498/18 , A61P25/28 , A61K31/4162
摘要： Compounds of formula (I): wherein R, X1, X2, X3, Z1, Z2, Z3, A and Ra are as defined in the description. Medicaments.

6. 发明申请

WO2017148925A1 RADIOLABELED MACROCYCLIC EGFR INHIBITOR 审中-公开
标题翻译：放射性标记的大环EGFR抑制剂
公开(公告)号：WO2017148925A1
公开(公告)日：2017-09-08
申请号：PCT/EP2017/054611
申请日：2017-02-28
申请人： ONCODESIGN SA
发明人： HOFLACK, Jan Marie Cyriel Jozef , BERTHET, Cyril , BLOM, Petra Marcella Françoise , VERCOUILLIE, Johnny , ROBIC, Caroline , CATOEN, Sarah
IPC分类号： A61K51/04 , C07D498/06 , A61K101/02
摘要： The present invention relates to 18-Fluor radiolabeled macrocyclic quinazoline compounds, which are suitable as positron emission tomography (PET) tracers for imaging epidermal growth factor receptors (EGFR), and their use in in vivo diagnosis, preclinical and clinical tumour imaging, patient stratification on the basis of mutational status of EGFR, and assessing tumour response to therapeutic treatments. The present invention also describes precursor compounds and methods of preparing the radiotracers. The invention is relevant to any cancer that is influenced or driven by deregulated EGFR, such as, but not limited to, non-small cell lung cancer (NSCLC), pancreatic, hepatocellular, oesophageal, gastric, colorectal, prostate, cervical, renal, ovarian, breast cancers, head and neck squamous cell carcinoma, and malignant glioma.
摘要翻译：本发明涉及18-Fluor放射性标记的大环喹唑啉化合物，其适合作为用于成像表皮生长因子受体（EGFR）的正电子发射断层扫描（PET）示踪剂，以及它们在<！ - SIPO < 体内诊断，临床前和临床肿瘤成像，基于EGFR突变状态的患者分层，以及评估肿瘤对治疗性治疗的响应。本发明还描述了前体化合物和制备该放射性示踪剂的方法。本发明涉及受去调节EGFR影响或驱动的任何癌症，例如但不限于非小细胞肺癌（NSCLC），胰腺癌，肝细胞癌，食管癌，胃癌，结肠直肠癌，前列腺癌，宫颈癌，肾癌，卵巢癌，乳腺癌，头颈部鳞状细胞癌和恶性胶质瘤。

7. 发明申请

WO2022194976A1 MACROCYCLIC LRRK2 KINASE INHIBITORS 审中-公开
公开(公告)号：WO2022194976A1
公开(公告)日：2022-09-22
申请号：PCT/EP2022/056910
申请日：2022-03-17
申请人： LES LABORATOIRES SERVIER , ONCODESIGN SA
发明人： DUMOULIN, Audrey , BLOM, Petra Marcella , DAUGAN, Alain , LAUGEOIS, Maxime , HOUSSEMAN, Christopher Gaétan , DENIS, Alexis , LAMOTTE, Yann , LE TIRAN, Arnaud , CHRISTENSEN, Kenneth
IPC分类号： C07D491/08 , C07D491/18 , C07D498/08 , C07D498/18 , C07D498/22 , C07D513/18 , A61P9/00 , A61P25/00 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/00 , A61P35/00 , A61P37/00 , A61K9/20 , A61K31/4162 , A61K31/4192 , A61K31/439
摘要： Compounds of formula (I) are useful as LRRK2 kinase inhibitors.

8. 发明申请

WO2016146651A1 MACROCYCLIC ACTIVIN-LIKE RECEPTOR KINASE INHIBITORS 审中-公开
标题翻译：大环激活素类受体激酶抑制剂
公开(公告)号：WO2016146651A1
公开(公告)日：2016-09-22
申请号：PCT/EP2016/055628
申请日：2016-03-16
申请人： ONCODESIGN SA
发明人： HOFLACK, Jan Marie Cyriel Jozef , BERTHET, Cyril , BENDERITTER, Pascal André René , BLOM, Petra Marcella Françoise , GOMEZ, Sylvie , DAOUBI, Mourad
IPC分类号： C07D487/18 , A61K31/529 , C07D498/18 , A61P19/08 , A61P35/00
CPC分类号： C07D487/18 , A61K31/519 , C07D498/18
摘要： The present invention relates to macrocyclic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of Activin-like receptor kinases, more in particular ALK1 and/or ALK2 and/or mutants thereof, for use in the diagnosis, prevention and/or treatment of ALK1-kinase and/or ALK2-kinase associated diseases. Moreover, the present invention provides methods of using said compounds, for instance as a medicine or diagnostic agent.
摘要翻译：本发明涉及大环化合物和含有作为激酶抑制剂的所述化合物的组合物，特别是作为激活素样受体激酶的抑制剂，更特别是ALK1和/或ALK2和/或其突变体的抑制剂，用于诊断，预防和 /或治疗ALK1激酶和/或ALK2-激酶相关疾病。此外，本发明提供使用所述化合物的方法，例如作为药物或诊断剂。

9. 发明授权

EP2970333B1 MACROCYCLIC LRRK2 KINASE INHIBITORS 有权
标题翻译： MAKROCYCLISCHE LRRK2-KASEASEHEMMER
公开(公告)号：EP2970333B1
公开(公告)日：2017-05-03
申请号：EP14709962
申请日：2014-03-14
申请人： IPSEN PHARMA SAS , ONCODESIGN SA
发明人： HOFLACK JAN , BLOM PETRA , LAVERGNE OLIVIER
IPC分类号： C07D498/18 , A61K31/437 , A61K31/504 , A61P25/16
CPC分类号： C07D498/18 , C07D487/18 , C07D498/22

10. 发明专利

SA517381087B1 مثبطات كيناز RIP2 حلقية ضخمة 未知
公开(公告)号：SA517381087B1
公开(公告)日：2021-02-09
申请号：SA517381087
申请日：2017-03-14
申请人： ONCODESIGN SA
发明人： PASCAL BENDERITTER , PETRA BLOM , JAN HOFLACK
摘要： يتعلقالاختراعالحاليبمركباتحلقيةضخمة macrocyclic وتركيباتتحتويعلىالمركباتالمذكورةتعملكمثبطاتكيناز kinase inhibitors ،وبخاصةمثبطات RIP2 و/أوطفراتها،للاستخدامفيتشخيص،الوقايةو/أوعلاجالأمراضالمرتبطةبكيناز kinase RIP2. علاوةعلىذلك،يوفرالاختراعالحاليطرقًالاستخدامالمركباتالمذكورة،كدواء medicine أوكعاملتشخيصيمثلًا diagnostic agent.

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