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公开(公告)号：EP3313405A1
公开(公告)日：2018-05-02
申请号：EP16741427.5
申请日：2016-06-22
发明人： COLLINS, Helen , DI PAOLO, Julie , KEEGAN, Kathy , KOZAKI, Ryohei , MEADOWS, Sarah , NELSON, Cara , QUEVA, Christophe , RAMANATHAN, Srinivasan , TANNHEIMER, Stacey , TUMAS, Daniel , YASUHIRO, Tomoko , YOSHIZAWA, Toshio
IPC分类号： A61K31/52 , A61K31/522 , A61K9/00 , A61P35/00 , A61P35/02
CPC分类号： A61K31/522 , A61K9/2004 , A61K31/52 , A61P35/00 , A61K2300/00
摘要： Provided herein are methods that relate to a therapeutic strategy for treatment of a B-cell malignancy. In particular, the methods include administration of a PI3K inhibitor and a BTK inhibitor.
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公开(公告)号：EP3355875A2
公开(公告)日：2018-08-08
申请号：EP16782161.0
申请日：2016-09-30
IPC分类号： A61K31/122 , A61K31/351 , A61K31/4748 , A61K31/522 , A61K31/675 , A61P35/00
CPC分类号： A61K31/522 , A61K31/122 , A61K31/351 , A61K31/4748 , A61K31/675 , A61K2300/00
摘要： Provided herein are methods relating to a therapeutic strategy for treatment of cancer, including hematological malignancies. In particular, the methods include administration of a Btk inhibitor and a checkpoint inhibitor, including combinations in which the Btk inhibitor is 6-amino-9-[(3R)-I-(2-butynoyl)-3- pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one, or a pharmaceutically acceptable salt thereof, and the checkpoint inhibitor is selected from inhibitors of PD-1, PD-L1, and CTLA-4.
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公开(公告)号：EP3415501B1
公开(公告)日：2020-04-08
申请号：EP18185739.2
申请日：2014-07-23
IPC分类号： C07D215/54 , C07D401/12 , C07D401/14 , A61K31/4709 , A61K31/5377 , A61P9/00 , A61P13/12 , A61P25/02 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/02 , A61P43/00
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公开(公告)号：EP3067356B1
公开(公告)日：2018-07-04
申请号：EP14859491.4
申请日：2014-11-06
发明人： INUKAI, Takayuki , TAKEUCHI, Jun , YASUHIRO, Tomoko , WOLF, Mark Allan , PAWAR, Vijay Dattaram , CHAKRABARTI, Anjan , CHITTIMALLA, Santhosh Kumar
IPC分类号： C07D487/04 , A61K31/519 , A61P9/00 , A61P13/12 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/02 , A61P43/00
CPC分类号： C07D487/04
摘要： The compound represented by general formula (I) has strong Axl inhibition activity by means of a pyridone ring structure being introduced into a pyrrolo pyrimidine skeleton, and so the result can serve as a treatment agent for Axl-related diseases, for example cancers such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glial tumors, renal disease, immune system disorders, and cardiovascular disease.
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公开(公告)号：EP3067356A1
公开(公告)日：2016-09-14
申请号：EP14859491.4
申请日：2014-11-06
发明人： INUKAI, Takayuki , TAKEUCHI, Jun , YASUHIRO, Tomoko , WOLF, Mark Allan , PAWAR, Vijay Dattaram , CHAKRABARTI, Anjan , CHITTIMALLA, Santhosh Kumar
IPC分类号： C07D487/04 , A61K31/519 , A61P9/00 , A61P13/12 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/02 , A61P43/00
CPC分类号： C07D487/04
摘要： The compound represented by general formula (I) has strong Axl inhibition activity by means of a pyridone ring structure being introduced into a pyrrolo pyrimidine skeleton, and so the result can serve as a treatment agent for Axl-related diseases, for example cancers such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glial tumors, renal disease, immune system disorders, and cardiovascular disease.
摘要翻译： 通式（I）表示的化合物通过将吡啶酮环结构引入吡咯并嘧啶骨架中而具有强Axl抑制活性，因此其结果可用作Axl相关疾病的治疗剂，例如癌症例如 急性骨髓性白血病，黑色素瘤，乳腺癌，胰腺癌和神经胶质瘤，肾病，免疫系统疾病和心血管疾病。
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公开(公告)号：EP3415501B9
公开(公告)日：2020-12-02
申请号：EP18185739.2
申请日：2014-07-23
IPC分类号： C07D215/54 , C07D401/12 , C07D401/14 , A61K31/4709 , A61K31/5377 , A61P9/00 , A61P13/12 , A61P25/02 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/02 , A61P43/00
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公开(公告)号：EP3239147B9
公开(公告)日：2020-01-08
申请号：EP15873185.1
申请日：2015-12-24
IPC分类号： C07D401/14 , A61K31/4709 , A61K31/517 , A61K31/55 , A61P7/02 , A61P9/00 , A61P9/10 , A61P13/12 , A61P17/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P35/02 , A61P35/04 , A61P43/00 , C07D471/04
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8.发明公开
公开(公告)号：EP3421039A1
公开(公告)日：2019-01-02
申请号：EP17756670.0
申请日：2017-02-24
发明人： TANAKA, Kohei , YASUHIRO, Tomoko
IPC分类号： A61K31/4709 , A61K39/395 , A61K45/00 , A61P35/00 , A61P43/00 , C07K16/18
摘要： The present invention addresses the problem of discovering and providing an effective cancer therapy by means of a drug. Provided is a drug for cancer therapy characterized by administering a combination between: a compound represented by a general formula (I) (wherein, all symbols are as described in the description), a salt thereof, a solvate thereof, an N-oxide thereof, or an Ax1 inhibitor as a prodrug of those; and an immune checkpoint inhibitor (e.g., anti-PD-1 antibody, etc.). The combination according to the present invention exerts a strong anti-tumor effect, and thereby is useful in cancer therapy.
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公开(公告)号：EP3026045A1
公开(公告)日：2016-06-01
申请号：EP14828976.2
申请日：2014-07-23
IPC分类号： C07D215/54 , A61K31/4709 , A61K31/5377 , A61P9/00 , A61P13/12 , A61P25/02 , A61P35/00 , A61P35/04 , A61P37/02 , A61P43/00 , C07D401/14
CPC分类号： C07D401/14 , C07D215/54 , C07D401/12
摘要： A compound represented by general formula (I):
has a strong Axl inhibitory activity by introducing a distinctive bicyclic structure in which a saturated carbon ring is fused to a pyridone ring, and can be a therapeutic agent for Axl-related diseases, for example, cancer such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glioma, kidney diseases, immune system diseases, and circulatory system diseases.摘要翻译： 由通式（I）表示的化合物：通过引入其中饱和碳环与吡啶酮环稠合的独特双环结构，具有强的Axl抑制活性，并且可以是Axl相关疾病的治疗剂，例如， 癌症如急性骨髓性白血病，黑素瘤，乳腺癌，胰腺癌和胶质瘤，肾脏疾病，免疫系统疾病和循环系统疾病。
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10.发明公开
公开(公告)号：EP3695839A1
公开(公告)日：2020-08-19
申请号：EP18866576.4
申请日：2018-10-12
IPC分类号： A61K31/4709 , A61K31/506 , A61P35/00 , A61P43/00 , C07D401/14
摘要： The present invention addresses the problem of finding an effective method for treating solid cancers and providing a pharmaceutical product therefor. The present invention provides a therapeutic agent for solid cancers, which contains N-{5-[(6, 7-dimethoxy-4-quinolinyl)oxy]-2-pyridinyl}-2, 5- dioxo-1-phenyl-1, 2, 5, 6, 7, 8-hexahydro-3-quinolinecarboxamide, a pharmaceutically acceptable salt thereof, or a hydrate of the compound or the salt as an active ingredient, and which is characterized by being administered in combination with osimertinib or a pharmaceutically acceptable salt thereof. The combination of the present invention exerts a strong antitumor effect, and is therefore useful for treatment of solid cancers.
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