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公开(公告)号:EP2364149A1
公开(公告)日:2011-09-14
申请号:EP09796056.1
申请日:2009-11-30
IPC分类号: A61K31/426 , C07D277/56 , A61P35/00
CPC分类号: C07D277/56 , A61K9/1652 , A61K9/2054 , A61K9/4858
摘要: The present invention relates to Traf2- and Nck-interacting kinase (TNIK) inhibitors, pharmaceutical compositions, and methods for the treatment of cancer patients with TNIK inhibitors. And the present invention relates to a novel aminothiazole derivatives. The TNIK inhibitors are showed by a next formula (I). (I) Wherein R1, R2, R3, R4, R5 and R6 represent independently a hydrogen atom or a substituent group.
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公开(公告)号:EP2364149B1
公开(公告)日:2014-05-07
申请号:EP09796056.1
申请日:2009-11-30
IPC分类号: A61K31/426 , C07D277/56 , A61P35/00
CPC分类号: C07D277/56 , A61K9/1652 , A61K9/2054 , A61K9/4858
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公开(公告)号:EP2855470B1
公开(公告)日:2018-10-17
申请号:EP13729492.2
申请日:2013-05-22
发明人: SAWA, Masaaki , MORIYAMA, Hideki , YAMADA, Tesshi , SHITASHIGE, Miki , KAWASE, Yusuke , UNO, Yuko
IPC分类号: C07D417/12 , C07D417/14 , C07D277/56 , A61K31/427 , A61P35/00
CPC分类号: C07D277/56 , C07D417/12 , C07D417/14
摘要: The present invention relates to novel bicyclic thiazole compounds that inhibit Traf2- and Nck-interacting kinase (TNIK), and as such are useful as TNIK inhibitors administered to cancer patients, especially to solid cancer patients such as colorectal cancer, pancreatic cancer, non-small cell lung cancer, prostate cancer or breast cancer. The bicyclic thiazole compounds are showed by a next formula (I). (wherein R1, R2, R3 and Q are as defined in the specification), or a pharmaceutically acceptable salt thereof.
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公开(公告)号:EP2855470A1
公开(公告)日:2015-04-08
申请号:EP13729492.2
申请日:2013-05-22
发明人: SAWA, Masaaki , MORIYAMA, Hideki , YAMADA, Tesshi , SHITASHIGE, Miki , KAWASE, Yusuke , UNO, Yuko
IPC分类号: C07D417/12 , C07D417/14 , C07D277/56 , A61K31/427 , A61P35/00
CPC分类号: C07D277/56 , C07D417/12 , C07D417/14
摘要: The present invention relates to novel bicyclic thiazole compounds that inhibit Traf2- and Nck-interacting kinase (TNIK), and as such are useful as TNIK inhibitors administered to cancer patients, especially to solid cancer patients such as colorectal cancer, pancreatic cancer, non-small cell lung cancer, prostate cancer or breast cancer. The bicyclic thiazole compounds are showed by a next formula (I). (wherein R1, R2, R3 and Q are as defined in the specification), or a pharmaceutically acceptable salt thereof.
摘要翻译: 本发明涉及抑制Traf2-和Nck相互作用激酶(TNIK)的新型双环噻唑化合物,并且因此可用作给予癌症患者的TNIK抑制剂,特别是用于固体癌症患者如结肠直肠癌,胰腺癌, 小细胞肺癌,前列腺癌或乳腺癌。 双环噻唑化合物由下式(I)表示。 (其中R 1,R 2,R 3和Q如说明书中所定义)或其药学上可接受的盐。
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公开(公告)号:EP3078660A1
公开(公告)日:2016-10-12
申请号:EP14868296.6
申请日:2014-12-05
IPC分类号: C07D403/12 , A61K31/517 , A61K31/5377 , A61P35/00 , A61P43/00 , C07D413/12 , C07D417/12
CPC分类号: C07D403/12 , C07D401/12 , C07D413/12 , C07D417/12
摘要: The present invention provides a quinazoline derivative represented by the following formula (I):
wherein R 1 and R 2 represent a hydrogen atom, a halogen atom, or a lower alkyl group optionally having a substituent; Z represents a cycloalkyl group having a substituent or a cycloalkenyl group having a substituent; and Q represents a bicyclic heteroaryl group optionally having a substituent, or a pharmaceutically acceptable salt thereof. Since the compound has an inhibitory effect on the Wnt/β-catenin signaling pathway and exhibits an antitumor effect, it is useful as a medicine.-
公开(公告)号:EP4373811A1
公开(公告)日:2024-05-29
申请号:EP22845500.2
申请日:2022-07-21
IPC分类号: C07D235/32 , C07D209/04 , C07D487/04 , A61K31/4184
CPC分类号: C07D403/12 , C07D471/04
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公开(公告)号:EP3042899A1
公开(公告)日:2016-07-13
申请号:EP14842654.7
申请日:2014-09-01
发明人: KAWAHATA, Wataru , ASAMI, Tokiko , SAWA, Masaaki , IRIE, Takayuki
IPC分类号: C07D401/10 , C07D401/14 , A61K31/506 , A61K31/5377 , A61P19/08 , A61P29/00 , A61P35/00 , A61P37/06
CPC分类号: C07D403/14 , C07D401/10 , C07D401/14
摘要: To provide a novel 2,6-diaminopyrimidine derivative by the following formula (I):
A 2,6-diaminopyrimidine derivative is represented by the formula (I):
wherein
R 1 represents a substituted or unsubstituted lower alkyl group, or a substituted or unsubstituted alkoxy group,
Ar represents a substituted or unsubstituted aryl group, or a substituted or unsubstituted heteroaryl group,
Z 1 and Z 2 represent carbon atoms, or either 1 or 2 of the Z 1 and Z 2 represent nitrogen atoms,
Q is selected from a structure (a) or (b) described below:
R 2 represents a substituted or unsubstituted lower alkyl group, or a substituted or unsubstituted cycloalkyl group,
R 3 represents a hydrogen atom or a halogen atom,
Y represents a nitrogen atom or a carbon atom, and
the bond drawn with a dotted line parallel to a solid line on structure (a) represents either double bond or single bond.摘要翻译: 通过下式(I)提供新的2,6-二氨基嘧啶衍生物:2,6-二氨基嘧啶衍生物由式(I)表示:其中R 1表示取代或未取代的低级烷基,或取代或未取代的 未取代的烷氧基,Ar表示取代或未取代的芳基或取代或未取代的杂芳基,Z 1和Z 2表示碳原子,或者1或2的Z 1和Z 2表示氮原子,Q选自 下述结构(a)或(b):R 2表示取代或未取代的低级烷基或取代或未取代的环烷基,R 3表示氢原子或卤素原子,Y表示氮原子或碳 原子,并且用结构(a)上平行于实线的虚线绘制的键表示双键或单键。
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公开(公告)号:EP4445902A2
公开(公告)日:2024-10-16
申请号:EP24190710.4
申请日:2020-12-18
发明人: SAWA, Masaaki , ARAI, Mai , NAKAI, Ryoko , MATSUMOTO, Hirokazu , PUGH, Catherine , HU, Eric , GUERRERO, Juan , JACOBSEN, Jesse , MEDLEY, Jonathan William , XU, Jie , LAD, Latesh , PATEL, Leena , GRAUPE, Michael , ZHU, Qingming , HOLMBO, Stephen , KOBAYASHI, Tetsuya , WATKINS, Will , MOAZAMI,, Yasamin , YEUNG, Suet C. , CODELLI, Julian A. , WEAVER, Heath A.
IPC分类号: A61K31/5415
摘要: The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents
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公开(公告)号:EP3533795A1
公开(公告)日:2019-09-04
申请号:EP17865551.0
申请日:2017-10-25
发明人: SAWA, Masaaki , ASAMITSU, Yuko , UNO, Yuko , OMURA, Satoshi , OTOGURO, Kazuhiko , IWATSUKI, Masato , ISHIYAMA, Aki , HOKARI, Rei
IPC分类号: C07D471/04 , A61K31/506 , A61K31/5377 , A61P33/06 , C07D491/056 , C07D491/107
摘要: The present invention provides a novel 2,4,6-substituted pyrimidine derivative, which is a compound represented by formula (I) (in the formula, ring A is a 6-membered heteroaryl group having at least one N atom optionally substituted with R1, R2, and R3; Z is an optionally substituted alkoxy group, an optionally substituted amino group, an optionally substituted heterocycloalkyl group, or an optionally substituted heteroaryl group; and R1, R2, and R3 are each independently selected from the group consisting of a hydrogen atom, a halogen atom, an optionally substituted alkyl group, an optionally substituted cycloalkyl group, an optionally substituted alkoxy group, an optionally substituted cycloalkyloxy group, an optionally substituted heterocycloalkyloxy group, an optionally substituted phenoxy group, an optionally substituted amino group, a nitro group, and a hydroxy group) or a pharmaceutically acceptable salt thereof.
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公开(公告)号:EP2824099A1
公开(公告)日:2015-01-14
申请号:EP13758233.4
申请日:2013-03-07
发明人: KAWAHATA, Wataru , ASAMI, Tokiko , SAWA, Masaaki , ASAMITSU, Yuko , IRIE, Takayuki , MIYAKE, Takahiro , KIYOI, Takao
IPC分类号: C07D251/42 , A61K31/53 , A61K31/5377 , A61P19/00 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/06 , A61P43/00
CPC分类号: C07D513/04 , A61K31/53 , A61K31/5377 , C07D251/18 , C07D251/22 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/04 , C07D495/04
摘要: To provide a novel triazine derivative represented by the following formula (I):
A triazine derivative represented by the following formula (I) :
wherein
R 1 represents a substituted or unsubstituted aryl group, a substituted or unsubstituted heterocyclic ring, a substituted or unsubstituted heterocyclic fused ring, or a substituted or unsubstituted alkynyl group,
R 2 represents a hydrogen atom, a halogen atom, a substituted or unsubstituted lower alkyl group, or a substituted or unsubstituted alkoxy group,
R 3 represents a substituted or unsubstituted aryl group, a substituted or unsubstituted heterocyclic ring, or a substituted or unsubstituted heterocyclic fused ring,
R 4 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted alkoxy group, a substituted or unsubstituted amino group, or a halogen atom, and
R 5 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, or R 1 and R 5 may be combined to form a saturated or unsaturated 5- to 6-membered ring, thereby forming a multiply fused ring,
or a pharmaceutically acceptable salt thereof.摘要翻译: 为了提供由下式(I)表示的新型三嗪衍生物:由下式(I)表示的三嗪衍生物:其中R1表示取代或未取代的芳基,取代或未取代的杂环,取代或未取代的杂环稠合 环或取代或未取代的炔基,R 2表示氢原子,卤素原子,取代或未取代的低级烷基或取代或未取代的烷氧基,R 3表示取代或未取代的芳基,取代或未取代的杂环 环或取代或未取代的杂环稠环,R 4表示氢原子,取代或未取代的低级烷基,取代或未取代的烷氧基,取代或未取代的氨基或卤素原子,R 5表示氢原子 ,取代或未取代的低级烷基,或者R 1和R 5可以结合形成饱和的 或不饱和的5至6元环,由此形成多重稠环或其药学上可接受的盐。
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