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公开(公告)号:US20200276180A1
公开(公告)日:2020-09-03
申请号:US16649455
申请日:2018-09-20
发明人: Hancheng ZHANG , Xiangyang YE
IPC分类号: A61K31/4709 , A61K39/395 , A61K31/47 , C07D215/14 , C07D405/12 , A61K31/5383 , C07D498/04 , C07D401/12 , A61K31/501 , A61K31/506 , C07D417/12 , C07D401/14
摘要: Compounds as IDO inhibitors and/or dual inhibitors of IDO-HDAC are described. Specifically, the compounds represented by the following formula (I) are described, wherein each group is defined as described in the specification. The compounds have IDO inhibitory activity or IDO-HDAC dual inhibitory activity and can be used for preventing or treating diseases associated with IDO and/or IDO-HDAC activity or expression levels. At the same time, the compounds of the present invention can be combined with an anti-tumor antibody such as PD-1 and PD-L1, and such a combination can greatly increase the anti-tumor response rate of the antibody and broaden the types of tumors to be treated.
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公开(公告)号:US20200270214A1
公开(公告)日:2020-08-27
申请号:US16634567
申请日:2019-07-26
发明人: Osman Güner , Bernard Lassegue , Kathy Griendling , Qian Xu , David Brown , J. Phillip Bowen , Amol Kulkarni , E. Blake Watkins
IPC分类号: C07D239/26 , C07D213/50 , C07D213/65 , C07D215/14 , C07D307/54
摘要: This disclosure relates to compounds and methods of treating or preventing a Nox related disease or condition comprising administering to a subject in need thereof a Nox inhibitor or pharmaceutical compositions comprising a Nox inhibitor disclosed herein, derivatives, or compounds disclosed herein optionally substituted with one or more substitutes including optional salt and prodrug forms. In certain embodiments, this disclosure relates to sulfonylurea compounds and uses reported herein.
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公开(公告)号:US20200239429A1
公开(公告)日:2020-07-30
申请号:US16652274
申请日:2018-11-15
发明人: Jiawang ZHU , Zhiquan SONG , Dong LONG , Lichun WANG , Jingyi WANG
IPC分类号: C07D401/04 , C07D333/56 , C07D215/14 , C07D215/227 , C07D215/38 , C07D413/04 , C07D215/36 , A61P1/16
摘要: The invention relates to an aromatic compound, pharmaceutical composition comprising the same, and a method for preparing the compound and an intermediate thereof. The invention also relates to use of the compound for the manufacture of a medicament for the prevention or treatment of a PPAR-related disease.
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公开(公告)号:US10709719B2
公开(公告)日:2020-07-14
申请号:US16188444
申请日:2018-11-13
发明人: Alaric J. Dyckman , T. G. Murali Dhar , Hai-Yun Xiao , John L. Gilmore , Michael G. Yang , Zili Xiao , David Marcoux
IPC分类号: A61K31/695 , C07F7/08 , A61K31/135 , C07D215/14 , C07D241/04 , C07C323/29 , C07C251/38 , C07C251/42 , C07C251/44 , C07D209/46 , C07D213/38 , C07C275/26 , C07C217/74 , C07C323/25 , C07C235/46 , C07F9/54 , C07F9/572 , C07F9/09 , C07C215/42 , C07C217/52 , C07C217/58 , C07C219/24 , C07C233/41 , C07C233/65 , C07C251/50 , C07C251/52 , C07C251/54 , C07C271/34 , C07C317/28 , C07C317/32 , C07C321/16 , C07C321/22 , C07C321/28 , C07D213/32 , C07D213/69 , C07D213/70 , C07D215/12 , C07D217/24 , C07D231/12 , C07D231/20 , C07D239/26 , C07D241/12 , C07D277/24 , C07D305/08 , C07D309/06 , C07D309/12 , C07D311/58 , C07D311/76 , C07D319/20 , C07D333/16 , C07F9/117 , C07F9/62 , C07F9/6503 , C07F9/6509 , C07F9/655 , C07F9/6553 , A61K31/137 , A61K31/15 , A61K31/165 , A61K31/166 , A61K31/17 , A61K31/222 , A61K31/24 , A61K31/27 , A61K31/337 , A61K31/351 , A61K31/352 , A61K31/381 , A61K31/415 , A61K31/4174 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/47 , A61K31/4965 , A61K31/505 , A61K31/661
摘要: Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1 is —OH or —OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
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公开(公告)号:US20200155538A1
公开(公告)日:2020-05-21
申请号:US16667306
申请日:2019-10-29
发明人: Peter A. Blomgren , Taryn Campbell , Jayaraman Chandrasekhar , Christopher T. Clark , Julian A. Codelli , Kevin S. Currie , Jeffrey E. Kropf , Yasamin Moazami , Nicole Nava , Leena Patel , Stephane Perreault , Jason K. Perry , Kassandra F. Sedillo , Natalie Seeger , Kirk L. Stevens , Jennifer Anne Treiberg , Suet C. Yeung , Zhongdong Zhao
IPC分类号: A61K31/47 , A61K45/06 , C07D215/14 , C07D401/10 , A61K31/4709 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D401/14 , C07D407/14 , A61K31/506 , A61K31/501 , A61K31/5355 , C07D413/12 , C07D417/12 , A61K31/541 , A61K31/517 , A61K31/4375 , C07D471/04 , C07D487/04 , A61K31/519
摘要: The present disclosure provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.
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公开(公告)号:US20200095214A1
公开(公告)日:2020-03-26
申请号:US16445768
申请日:2019-06-19
IPC分类号: C07D295/192 , C07C237/22 , C07D213/81 , C07D233/90 , C07D295/185 , C07D295/26 , A61K31/166 , A61K31/40 , A61K31/4453 , A61K31/454 , A61K31/4545 , A61K31/47 , A61K31/495 , A61K31/5375 , A61K31/54 , C07D215/14
摘要: Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.
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公开(公告)号:US20190375737A1
公开(公告)日:2019-12-12
申请号:US16436843
申请日:2019-06-10
申请人: Russell Dahl
发明人: Russell Dahl
IPC分类号: C07D409/06 , C07D215/06 , A61P3/10 , C07D215/14
摘要: Provided herein are compounds of Formula I, pharmaceutical compositions thereof, and methods of their use for treating, preventing, or ameliorating one or more symptoms of a neurological disease, neurodegenerative disorder, or diabetes.
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公开(公告)号:US20190367508A1
公开(公告)日:2019-12-05
申请号:US16443929
申请日:2019-06-18
IPC分类号: C07D471/04 , A61K31/4427 , A61P25/28 , C07D401/14 , C07D213/74 , C07D309/18 , C07D401/04 , C07D237/08 , A61K31/50 , C07C233/25 , C07D213/30 , C07D213/34 , C07D213/57 , C07D213/61 , C07D213/64 , C07D213/73 , C07D213/75 , C07D213/80 , C07D215/14 , C07D239/26 , C07D309/22 , C07D413/10
摘要: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
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公开(公告)号:US10457655B2
公开(公告)日:2019-10-29
申请号:US15786539
申请日:2017-10-17
发明人: Kenneth W. Bair , David R. Lancia, Jr. , Hongbin Li , James Loch , Wei Lu , Matthew W. Martin , David S. Millan , Shawn E.R. Schiller , Mark J. Tebbe
IPC分类号: C07D295/192 , A61K31/4965 , A61P35/00 , C07D401/04 , C07D403/04 , C07D405/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D471/04 , C07D487/04 , C07D491/048 , C07D495/04 , C07D213/65 , C07D213/69 , C07D213/56 , C07D231/12 , C07D235/08 , C07D209/08 , C07D209/18 , C07D263/57 , C07D271/12 , C07D277/66 , C07D277/62 , C07D513/04 , A61K31/495 , A61K31/496 , A61K31/4985 , A61K31/5025 , A61K31/506 , A61K45/06 , C07D215/14 , C07D231/56 , C07D257/04 , C07D305/08 , A61K31/497 , C07D217/16
摘要: The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:
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公开(公告)号:US20190322617A1
公开(公告)日:2019-10-24
申请号:US16405581
申请日:2019-05-07
发明人: Ya-Huei Kuo , Wei-Jan Huang , Chung-I Chang
IPC分类号: C07C259/06 , C07D217/20 , C07D209/18 , C07D209/08 , C07D333/24 , C07D213/56 , C07D217/16 , C07D215/14 , C07D213/74 , C07D307/91 , C07D317/60
摘要: Provided herein, inter alia, are compound and methods of treating cancer by inhibiting HDAC8.
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