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公开(公告)号：US20200071297A1
公开(公告)日：2020-03-05
申请号：US16469071
申请日：2017-12-07
Applicant: Boehringer Ingelheim International GmbH
Inventor： Steffen STEURER , Georg DAHMANN , Nina KERRES (Deceased) , Manfred KOEGL
IPC: C07D401/14 , C07D498/08 , C07D413/14 , C07D471/04 , C07D491/113 , C07D417/14 , A61P35/00
Abstract: The present invention encompasses compounds of formula (I), wherein the groups R1 to R5, X, Y and W have the meanings given in the claims and specification, their use as inhibitors of BCL6, pharmaceutical compositions which contain compounds of this kind and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.
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公开(公告)号：US20200016111A1
公开(公告)日：2020-01-16
申请号：US16524498
申请日：2019-07-29
Applicant: Alkermes Pharma Ireland Limited
Inventor： Tarek A. Zeidan , Scott Duncan , Christopher P. Hencken , Thomas Andrew Wynn , Carlos N. Sanrame
IPC: A61K31/225 , C07D491/113 , C07C317/28 , C07D211/38 , C07D295/088 , C07D207/40 , C07D211/06 , C07D207/06 , C07D209/52 , C07C317/18 , C07C219/08 , C07C229/16 , C07C233/18 , C07C233/91
Abstract: The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.
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公开(公告)号：US10519137B2
公开(公告)日：2019-12-31
申请号：US15810521
申请日：2017-11-13
Applicant: ASTEX THERAPEUTICS LTD
Inventor： Gordon Saxty , Christopher William Murray , Valerio Berdini , Gilbert Ebai Besong , Steven John Woodhead , Michael Reader , Laurence Anne Mevellec , Patrick René Angibaud , Eddy Jean Edgard Freyne , Timothy Pietro Suren Perera , Berthold Wroblowski , Alexandra Papanikos , Olivier Alexis Georges Querolle , Isabelle Noëlle Constance Pilatte , Pascal Ghislain André Bonnet , Werner Constant Johan Embrechts , Rhalid Akkari , Lieven Meerpoel
IPC: C07D231/10 , C07D231/12 , A61K31/415 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D487/08 , A61K31/498 , A61K31/5377 , A61K45/06 , C07D491/113 , C07D401/14 , C07F9/6524
Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
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公开(公告)号：US10428095B2
公开(公告)日：2019-10-01
申请号：US16148622
申请日：2018-10-01
Applicant: Achillion Pharmaceuticals, Inc.
Inventor： Jason Allan Wiles , Avinash S. Phadke , Xiangzhu Wang , Dawei Chen , Akihiro Hashimoto , Venkat Rao Gadhachanda , Godwin Pais , Qiuping Wang , Atul Agarwal , Milind Deshpande
IPC: C07D403/14 , C07F9/572 , C07D209/42 , C07D403/12 , C07D401/14 , C07D471/04 , C07D417/06 , C07D403/06 , C07D417/14 , C07F7/08 , C07D413/14 , C07D487/04 , C07D405/14 , C07D403/08 , C07D413/06 , C07F5/02 , C07F9/6561 , C07F9/6558 , A61K31/404 , A61K31/407 , A61K31/4162 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/437 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/549 , A61K31/55 , A61K31/675 , A61K31/683 , C07B59/00 , C07D209/14 , C07D209/40 , C07D405/12 , C07D417/12 , C07D487/14 , C07D491/113 , C07D495/04 , C07D513/04 , A61K9/00 , A61K31/4045 , A61K31/444 , A61K31/501 , A61K31/519 , C07D209/12 , C07D209/30 , C07D209/44 , C07D209/88 , C07D471/08
Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.
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公开(公告)号：US20190270744A1
公开(公告)日：2019-09-05
申请号：US16290174
申请日：2019-03-01
Applicant: Reaction Biology Corp.
Inventor： Haiching Ma , Yangbo Feng , Yuren Wang
IPC: C07D471/10 , C07D498/10 , C07D491/113 , C07D491/107
Abstract: The present invention relates to methods of modulating activity of histone deacetylases (HDACs). The present invention also relates to methods of treating HDAC-associated diseases including, but not limited to, cancers, inflammatory disorders, and neurodegenerative disorders. The present invention also provides novel compounds and compositions thereof and methods of preparation of the same. The present invention also includes methods of inhibiting HDACs, and methods of treating HDAC-associated diseases using the compounds of the invention.
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公开(公告)号：US10399992B2
公开(公告)日：2019-09-03
申请号：US16087308
申请日：2017-03-28
Applicant: Zhejiang Hisun Pharmaceutical Co., Ltd.
Inventor： Jinqing Zhong , Xuyang Zhao , Hua Bai , Yongxiang Gong , Xinlong Zhang , Qifeng Zhu , Weiwei Liu , Ya Zhou
IPC: C07D491/056 , C07D491/113 , A61P25/28
Abstract: Disclosed are a method for preparing a benzodioxole derivative (AD-35) shown by Formula (I) and an intermediate thereof. The method of the present invention involves: using piperic acid as a raw material; and performing bromination, esterification, cyanidation, cyclopropane lactamization, amide nitrogen alkylation, deprotection, piperidine nitrogen alkylation and salification to obtain the compound of Formula (I). The method has cheap and easily available start raw materials, short synthesis routes and simple operation, and is suitable for industrial production.
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公开(公告)号：US10344019B2
公开(公告)日：2019-07-09
申请号：US14814392
申请日：2015-07-30
Applicant: GILEAD PHARMASSET LLC
Inventor： Elizabeth M. Bacon , Jeromy J. Cottell , Ashley Anne Katana , Darryl Kato , Evan S. Krygowski , John O. Link , James G. Taylor , Chinh Tran , Teresa Alejandra Trejo Martin , Zheng-Yu Yang , Sheila M. Zipfel
IPC: C07D403/14 , C07D405/14 , A61K31/4178 , A61K45/06 , A61K31/4184 , A61K31/4188 , C07D417/14 , C07D471/08 , C07D491/10 , C07D493/04 , C07D495/04 , C07D513/04 , A61K31/5377 , C07D491/107 , C07D491/113
Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
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28.发明申请
公开(公告)号：US20190185498A1
公开(公告)日：2019-06-20
申请号：US16276139
申请日：2019-02-14
Applicant: Achillion Pharmaceuticals, Inc.
Inventor： Jason Allan Wiles , Venkat Rao Gadhachanda , Qiuping Wang , Godwin Pais , Akihiro Hashimoto , Dawei Chen , Xiangzhu Wang , Atul Agarwal , Milind Deshpande , Avinash S. Phadke
IPC: A61K31/683 , C07F9/572 , C07D417/06 , C07F7/08 , C07D401/14 , C07D403/14 , C07D403/12 , C07D209/42 , C07D471/08 , C07D209/30 , C07D209/44 , C07D209/88 , C07D209/12 , A61K31/519 , A61K31/501 , A61K9/00 , A61K31/4045 , A61K31/444 , A61K31/675 , A61K31/404 , A61K31/407 , A61K31/4162 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/437 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/549 , A61K31/55 , C07F9/6558 , C07F9/6561 , C07D513/04 , C07B59/00 , C07D471/04 , C07D209/14 , C07D209/40 , C07D405/12 , C07D417/12 , C07D487/14 , C07D491/113 , C07D495/04 , C07D413/06 , C07D403/08 , C07D405/14 , C07D487/04 , C07D413/14 , C07D417/14 , C07D403/06 , C07F5/02
Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.
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公开(公告)号：US10202353B2
公开(公告)日：2019-02-12
申请号：US15121643
申请日：2015-02-26
Applicant: Gilead Sciences, Inc.
Inventor： Steven S. Bondy , Chien-Hung Chou , John O. Link , Winston C. Tse
IPC: C07D403/12 , C07D231/56 , C07D231/54 , C07D401/12 , C07D409/12 , C07D417/12 , C07D491/10 , A61K31/357 , A61K31/416 , A61K31/4162 , A61K31/4178 , A61K31/427 , A61K31/4439 , A61K31/522 , A61K45/06 , C07D319/08 , C07D405/12 , C07D473/06 , C07D491/113
Abstract: Compounds of Formula I, or salts thereof, are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of Formula I, processes for preparing compounds of Formula I, intermediates useful for preparing compounds of Formula I and therapeutic, methods for treating a Retroviridae viral infection, in particular infection caused by the HIV virus.
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公开(公告)号：US20180291047A1
公开(公告)日：2018-10-11
申请号：US16006533
申请日：2018-06-12
Applicant: Achillion Pharmaceuticals, Inc.
Inventor： Jason Allan Wiles , Godwin Pais , Akihiro Hashimoto , Venkat Rao Gadhachanda , Qiuping Wang , Dawei Chen , Xiangzhu Wang , Atul Agarwal , Milind Deshpande , Avinash S. Phadke
IPC: C07F9/572 , C07D417/06 , C07F7/08 , C07D401/14 , C07D403/14 , C07D403/12 , C07D209/42 , C07D471/08 , C07D209/30 , C07D209/44 , C07D209/88 , C07D209/12 , A61K31/519 , A61K31/501 , A61K9/00 , A61K31/4045 , A61K31/444 , A61K31/675 , A61K31/404 , A61K31/407 , A61K31/4162 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/437 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/549 , A61K31/55 , A61K31/683 , C07F9/6558 , C07F9/6561 , C07D513/04 , C07B59/00 , C07D209/14 , C07D209/40 , C07D405/12 , C07D417/12 , C07D487/14 , C07D491/113 , C07D495/04 , C07D413/06 , C07D403/08 , C07D405/14 , C07D487/04 , C07D413/14 , C07D417/14 , C07D403/06 , C07F5/02 , C07D471/04
Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof, wherein R12 or R13 on the A group is an alkyne (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.
