- ANTIVIRAL COMPOUNDS
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Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus v
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Paragraph 0637; 0638
(2016/09/26)
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- ANTIVIRAL COMPOUNDS
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Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).
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Paragraph 1272
(2015/03/13)
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- Discovery of dual leucine zipper kinase (DLK, MAP3K12) inhibitors with activity in neurodegeneration models
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Dual leucine zipper kinase (DLK, MAP3K12) was recently identified as an essential regulator of neuronal degeneration in multiple contexts. Here we describe the generation of potent and selective DLK inhibitors starting from a high-throughput screening hit. Using proposed hinge-binding interactions to infer a binding mode and specific design parameters to optimize for CNS druglike molecules, we came to focus on the di(pyridin-2-yl)amines because of their combination of desirable potency and good brain penetration following oral dosing. Our lead inhibitor GNE-3511 (26) displayed concentration-dependent protection of neurons from degeneration in vitro and demonstrated dose-dependent activity in two different animal models of disease. These results suggest that specific pharmacological inhibition of DLK may have therapeutic potential in multiple indications.
- Patel, Snahel,Cohen, Frederick,Dean, Brian J.,De La Torre, Kelly,Deshmukh, Gauri,Estrada, Anthony A.,Ghosh, Arundhati Sengupta,Gibbons, Paul,Gustafson, Amy,Huestis, Malcolm P.,Le Pichon, Claire E.,Lin, Han,Liu, Wendy,Liu, Xingrong,Liu, Yichin,Ly, Cuong Q.,Lyssikatos, Joseph P.,Ma, Changyou,Scearce-Levie, Kimberly,Shin, Young G.,Solanoy, Hilda,Stark, Kimberly L.,Wang, Jian,Wang, Bei,Zhao, Xianrui,Lewcock, Joseph W.,Siu, Michael
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p. 401 - 418
(2015/01/30)
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- SUBSTITUTED DIPYRIDYLAMINES AND USES THEREOF
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The present invention provides for compounds of Formula I and various embodiments thereof, and compositions comprising compounds of Formula I and various embodiments thereof. In compounds of Formula I, the groups R1, R2, R3, R4, R5, R6, m, n and the C-linked Ring have the meaning as described herein. The present invention also provides for methods of using compounds of Formula I and compositions comprising compounds of Formula I as DLK inhibitors and for treating neurodegeneration diseases and disorders.
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Page/Page column 200
(2014/01/07)
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- AMINOPYRAZINE DERIVATIVE AND MEDICINE
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The present invention relates to a compound represented by general formula [1] satisfying the following (I) or (II), or a pharmaceutical acceptable salt of the compound. (I) X is CH or N; R1 is a halogen atom,; and R2 is H, a halogen atom, CN, [2], [3], [8], [9], an —O-alkyl, an —O-(saturated ring), etc. [2]: —C(RC)(RD)(RE) (RC to RE each are H, an alkyl, etc.) [3]: —N(RF)(RG) (RF and RG each are H, OH, amino, a (hetero)aryl, etc.) [8]: —C(═O)RL (RL is an alkyl, OH, an alkoxy, amino, etc.) [9]: a (substituted)phenyl; (II) X is >C—C(—O)R3 (R3 is a (substituted)amino, an alkoxy, OH, etc.); R1 is a halogen atom; R2 is H; R3 is H or OH; and R3 and R4 each are H or an alkyl.
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Page/Page column 60
(2011/12/12)
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