- ASK1 inhibitor and application thereof
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The invention relates to compounds represented by a general formula (I) shown in the specification, a pharmaceutically acceptable salt and ester, or a stereoisomer of the compounds. The invention alsorelates to a preparation method of the compounds, a pharmaceutical preparation and a pharmaceutical composition containing the compounds. The compounds provided by the invention can effectively inhibit the amino acid phosphorylation of ASK1 and inhibit the activation of the ASK1; therefore, the compounds can treat and/or prevent ASK1-mediated diseases and related diseases.
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Paragraph 0138-0142
(2020/02/10)
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- NOVEL OXALYL PIPERAZINES ACTIVE AGAINST THE HEPATITIS B VIRUS (HBV)
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The present invention relates generally to novel antiviral agents. Specifically, the present invention relates to compounds which can inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV replication cycle, compositions comprising such compounds, methods for inhibiting HBV viral replication, methods for treating or preventing HBV infection, and processes and intermediates for making the compounds.
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Page/Page column 98-99
(2020/11/12)
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- NOVEL INDOLIZINE-2-CARBOXAMIDES ACTIVE AGAINST THE HEPATITIS B VIRUS (HBV)
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The present invention relates generally to novel antiviral agents. Specifically, the present invention relates to compounds which can inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV replication cycle, compositions comprising such compounds, methods for inhibiting HBV viral replication, methods for treating or preventing HBV infection, and processes and intermediates for making the compounds.
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Page/Page column 101-102
(2020/11/12)
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- Neurotrophic factor tyrosine kinase receptor inhibitor
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The invention provides a neurotrophic factor tyrosine kinase receptor inhibitor. The tyrosine kinase receptor inhibitor provided by the invention has a tricyclic parent core structure, can inhibit theactivity of Trk kinase and can be used for treating mammalian diseases mediated by the Trk kinase.
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Paragraph 0628; 0630-0632
(2018/05/30)
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- PROCESS FOR FLUORINATING COMPOUNDS
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Methods of preparing a fluorinated aryl or heteroaryl substrate by combining a quaternary ammonium cyanide and an aryl or heteroaryl substrate substituted with at least one chloro, bromo, sulfonyl, or nitro group to thereby provide a mixture, and combining the mixture with hexafluorobenzene to thereby provide the fluorinated substrate.
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Paragraph 0087; 0090
(2015/05/26)
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- Mild fluorination of chloropyridines with in situ generated anhydrous tetrabutylammonium fluoride
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This paper describes the fluorination of nitrogen heterocycles using anhydrous NBu4F. Quinoline derivatives as well as a number of 3- and 5-substituted pyridines undergo high-yielding fluorination at room temperature using this reagent. These results with anhydrous NBu4F compare favorably to traditional halex fluorinations using alkali metal fluorides, which generally require temperatures of ≥100 °C.
- Allen, Laura J.,Muhuhi, Joseck M.,Bland, Douglas C.,Merzel, Rachel,Sanford, Melanie S.
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p. 5827 - 5833
(2014/07/08)
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- Pd-catalyzed nucleophilic fluorination of aryl bromides
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On the basis of mechanism-driven reaction design, a Pd-catalyzed nucleophilic fluorination of aryl bromides and iodides has been developed. The method exhibits a broad substrate scope, especially with respect to nitrogen-containing heteroaryl bromides, and proceeds with minimal formation of the corresponding reduction products. A facilitated ligand modification process was shown to be critical to the success of the reaction.
- Lee, Hong Geun,Milner, Phillip J.,Buchwald, Stephen L.
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supporting information
p. 3792 - 3795
(2014/04/03)
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- NOVEL COMPOUNDS
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This invention relates to compounds of formula (I) their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.
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Page/Page column 46
(2013/06/27)
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- NOVEL COMPOUNDS
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This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.
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Paragraph 0239; 0240; 0241
(2013/06/05)
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- FUSED PHENYL AMIDO HETEROCYCLIC COMPOUNDS FOR THE PREVENTION AND TREATMENT OF GLUCOKINASE-MEDIATED DISEASES
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The present invention relates to a compound of formula (I): (I); or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: B(i); and B(i
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Page/Page column 124
(2008/06/13)
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- 2-(2-imidazolin-2-yl)-pyridines and quinolines, process and intermediates for the preparation thereof, and use of said compounds as herbicidal agents
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There are provided novel 2-(2-imidazolin-2-yl)pyridine and quinoline compounds, a process and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and perennial plant species therewith.
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