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1. 发明授权

US09682961B2 Quinazoline derivative 有权
公开(公告)号：US09682961B2
公开(公告)日：2017-06-20
申请号：US14890868
申请日：2014-12-05
申请人： CARNA BIOSCIENCES, INC. , NATIONAL CANCER CENTER
发明人： Hideki Moriyama , Masaaki Sawa , Yuko Uno , Shigeki Kashimoto , Tesshi Yamada
IPC分类号： C07D403/12 , C07D413/12 , C07D417/12 , C07D401/12
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 R1 and R2 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.

2. 发明申请

US20160221991A1 NOVEL TRIAZINE DERIVATIVE 审中-公开
标题翻译：新的TRIAZINE DERIVATIVE
公开(公告)号：US20160221991A1
公开(公告)日：2016-08-04
申请号：US15022974
申请日：2014-09-12
申请人： CARNA BIOSCIENCES, INC.
发明人： Takahiro MIYAKE , Wataru KAWAHATA , Tokiko ASAMI , Masaaki SAWA
IPC分类号： C07D401/14
CPC分类号： C07D401/14
摘要： To provide a novel triazine derivative represented by the following formula (I): A triazine derivative represented by the following formula (I): wherein R1 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, either of Z1 and Z2 represents carbon atom and the other is nitrogen atom, or both of the Z1 and Z2 represent nitrogen atoms, Q is selected from a structure (a) and (b) described below: wherein R2 represents a substituted or unsubstituted lower alkyl group, or a substituted or unsubstituted cycloalkyl group, R3 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, or a pharmaceutically acceptable salt thereof.
摘要翻译：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低级烷基或取代或未取代的烷氧基，Ar表示取代或未取代的芳基或取代或未取代的杂芳基，Z1和Z2中的任一个表示碳原子，另一个是氮原子，或者Z1和Z2都表示氮原子，Q选自结构（a）和（ b）如下所述：其中R2表示取代或未取代的低级烷基或取代或未取代的环烷基，R3表示氢原子或卤素原子，Y表示氮原子或碳原子，并且用平行于结构（a）上的实线的虚线表示双键或单键，或其药学上可接受的盐。

3. 发明申请

US20150011751A1 NOVEL TRIAZINE DERIVATIVE 审中-公开
标题翻译：新的TRIAZINE DERIVATIVE
公开(公告)号：US20150011751A1
公开(公告)日：2015-01-08
申请号：US14383860
申请日：2013-03-07
申请人： CARNA BIOSCIENCES, INC.
发明人： Wataru Kawahata , Tokiko Asami , Masaaki Sawa , Yuko Asamitsu , Takayuki Irie , Takahiro Miyake , Takao Kiyoi
IPC分类号： C07D513/04 , C07D401/14 , C07D251/22 , C07D401/12 , C07D409/12 , C07D413/14 , C07D405/12 , C07D487/04 , C07D417/12 , C07D251/18 , C07D403/10
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 R1 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, R2 represents a hydrogen atom, a halogen atom, a substituted or unsubstituted lower alkyl group, or a substituted or unsubstituted alkoxy group, R3 represents a substituted or unsubstituted aryl group, a substituted or unsubstituted heterocyclic ring, or a substituted or unsubstituted heterocyclic fused ring, R4 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 R5 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, or R1 and R5 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：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合环，R4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，R5表示氢原子，取代或未取代的低级烷基，或R 1和R 5可以组合形成饱和的o r不饱和5-至6-元环，从而形成多稠环，或其药学上可接受的盐。

4. 发明公开

US20240182476A1 DIACYLGLYCEROL KINASE MODULATING COMPOUNDS 审中-公开
公开(公告)号：US20240182476A1
公开(公告)日：2024-06-06
申请号：US18450646
申请日：2023-08-16
申请人： GILEAD SCIENCES, INC. , CARNA BIOSCIENCES, INC.
发明人： Masaaki Sawa , Mai Arai , Ryoko Nakai , Hirokazu Matsumoto , Catherine Pugh , Eric Hu , Juan Guerrero , Jesse Jacobsen , Jonathan William Medley , Jie Xu , Latesh Lad , Leena Patel , Michael Graupe , Qingming Zhu , Stephen Holmbo , Tetsuya Kobayashi , Will Watkins , Yasamin Moazami , Suet C. Yeung , Julian A. Codelli , Heath A. Weaver
IPC分类号： C07D487/04 , A61K31/395 , A61K31/519 , A61K31/5377 , A61K31/538 , A61K31/55 , A61K31/553 , A61K31/695 , A61K31/704 , A61K31/7068 , A61K35/15 , A61K35/17 , A61K39/395 , A61K45/06 , C07D519/00 , C07F7/18
CPC分类号： C07D487/04 , A61K31/519 , A61K31/5377 , A61K31/538 , A61K31/55 , A61K31/553 , A61K31/5545 , A61K31/695 , A61K31/704 , A61K31/7068 , A61K35/15 , A61K35/17 , A61K39/3955 , A61K45/06 , C07D519/00 , C07F7/1804
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.

5. 发明申请

US20160264555A1 NOVEL QUINAZOLINE DERIVATIVE 有权
标题翻译：新的喹诺酮衍生物
公开(公告)号：US20160264555A1
公开(公告)日：2016-09-15
申请号：US14890868
申请日：2014-12-05
申请人： CARNA BIOSCIENCES, INC. , NATIONAL CANCER CENTER
发明人： Hideki MORIYAMA , Masaaki SAWA , Yuko UNO , Shigeki KASHIMOTO , Tesshi YAMADA
IPC分类号： C07D403/12 , C07D413/12 , C07D401/12 , 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 R1 and R2 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.
摘要翻译：其中R1和R2表示氢原子，卤素原子或任选具有取代基的低级烷基; Z表示具有取代基的环烷基或具有取代基的环烯基; 和Q表示任选具有取代基的双环杂芳基，或其药学上可接受的盐。由于该化合物对Wnt /β-连环蛋白信号通路具有抑制作用并具有抗肿瘤作用，因此作为药物是有用的。

6. 发明授权

US12037325B2 1,2-diaminobenzimidazole derivative 有权
公开(公告)号：US12037325B2
公开(公告)日：2024-07-16
申请号：US17870303
申请日：2022-07-21
申请人： Carna Biosciences, Inc.
发明人： Hirokazu Matsumoto , Takao Kiyoi , Shiori Takamatsu , Masaaki Sawa
IPC分类号： C07D235/30 , A61K31/437 , C07D403/12 , C07D471/04
CPC分类号： C07D403/12 , C07D471/04 , C07B2200/05
摘要： Provided herein are novel compounds having an inhibitory effect on the activation of a STING pathway. The provided compounds are 1,2-diaminobenzimidazole derivatives represented by a compound formula (I) or a pharmaceutically acceptable salt thereof:

wherein A1, A2, R1, R2, R3, R4, and R5 are defined in the specification.

7. 再颁专利

USRE48140E1 Furanone derivative 有权
公开(公告)号：USRE48140E1
公开(公告)日：2020-08-04
申请号：US15967323
申请日：2018-04-30
申请人： Carna Biosciences, Inc.
发明人： Takayuki Irie , Ayako Sawa , Masaaki Sawa , Tokiko Asami , Yoko Funakoshi , Chika Tanaka
IPC分类号： C07D471/04 , A61K31/437 , A61K31/4375 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/506 , C07D519/00 , A61K31/5355 , A61K31/541
CPC分类号： C07D471/04 , A61K31/437 , A61K31/4375 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/5355 , A61K31/541 , C07D519/00
摘要： To provide a novel furanone derivative, and a medicine including the same. The furanone derivative is represented by the formula (I):

wherein A represents —COOR1 or a hydrogen atom; R1 represents a hydrogen atom, an optionally substituted hydrocarbon group, or an optionally substituted heterocycle; R2 and R3 are the same or different and each independently represent a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted phenyl group, an optionally substituted heterocycle, an optionally substituted heterocyclic fused ring, or an optionally substituted amino group; or alternatively, R2 and R3, taken together with the nitrogen atom to which they are attached, may form an optionally substituted heterocycle or an optionally substituted heterocyclic fused ring; and R4 represents a hydrogen atom or a halogen atom; with the proviso that when A represents —COOR1, R2 and R3 are not optionally substituted amino groups at the same time, and when A represents a hydrogen atom, R3 represents a hydrogen atom.

8. 发明授权

US10538521B2 Pyrimidine derivative having antimalarial activity 有权
公开(公告)号：US10538521B2
公开(公告)日：2020-01-21
申请号：US16344471
申请日：2017-10-25
申请人： CARNA BIOSCIENCES, INC. , THE KITASATO INSTITUTE
发明人： Masaaki Sawa , Yuko Asamitsu , Yuko Uno , Satoshi Omura , Kazuhiko Otoguro , Masato Iwatsuki , Aki Ishiyama , Rei Hokari
IPC分类号： C07D471/04 , A61P33/06 , A61K31/506
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.

9. 发明申请

US20190359616A1 NOVEL OXOISOQUINOLINE DERIVATIVES 审中-公开
公开(公告)号：US20190359616A1
公开(公告)日：2019-11-28
申请号：US16463493
申请日：2017-11-24
申请人： CARNA BIOSCIENCES, INC.
发明人： Wataru KAWAHATA , Takao KIYOI , Takayuki IRIE , Tokiko ASAMI , Masaaki SAWA , Shigeki KASHIMOTO
IPC分类号： C07D487/04 , C07D473/00
摘要： The present invention provides with an oxoisoquinoline derivative represented by the formula (I) (in the formula, Q and R1 are as defined in the description) or a pharmaceutically acceptable salt thereof, which is useful as a Bruton's kinase inhibitor for treating cancer, B-cell lymphoma, chronic lymphocytic leukemia and the like.

10. 再颁专利

USRE46815E1 Furanone derivative 有权
公开(公告)号：USRE46815E1
公开(公告)日：2018-05-01
申请号：US15172021
申请日：2016-06-02
申请人： Carna Biosciences, Inc.
发明人： Takayuki Irie , Ayako Sawa , Masaaki Sawa , Tokiko Asami , Yoko Funakoshi , Chika Tanaka
IPC分类号： C07D471/02 , C07D491/02 , C07D498/02 , C07D515/02 , C07D513/02 , C07D471/04 , A61K31/4375 , A61K31/444 , A61K31/4545 , A61K31/4709 , C07D519/00 , A61K31/506 , A61K31/5355 , A61K31/541 , A61K31/437 , A61K31/496
CPC分类号： C07D471/04 , A61K31/437 , A61K31/4375 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/5355 , A61K31/541 , C07D519/00
摘要： To provide a novel furanone derivative, and a medicine including the same. The furanone derivative is represented by the formula (I): wherein A represents —COOR1 or a hydrogen atom; R1 represents a hydrogen atom, an optionally substituted hydrocarbon group, or an optionally substituted heterocycle; R2 and R3 are the same or different and each independently represent a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted phenyl group, an optionally substituted heterocycle, an optionally substituted heterocyclic fused ring, or an optionally substituted amino group; or alternatively, R2 and R3, taken together with the nitrogen atom to which they are attached, may form an optionally substituted heterocycle or an optionally substituted heterocyclic fused ring; and R4 represents a hydrogen atom or a halogen atom; with the proviso that when A represents —COOR1, R2 and R3 are not optionally substituted amino groups at the same time, and when A represents a hydrogen atom, R3 represents a hydrogen atom.

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