209798-48-1Relevant articles and documents
CDK8/19 INHIBITORS
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Paragraph 0095, (2021/06/10)
The present invention relates to novel compounds of formula I: which have the properties of CDK8/19 inhibitors, to a pharmaceutical composition comprising said compounds, and to use thereof as a medicine for treating diseases and disorders.
POLYHETEROCYCLIC COMPOUNDS AS METTL3 INHIBITORS
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Page/Page column 335, (2021/06/11)
The present invention relates to compounds of formula (I) that function as inhibitors of METTL3 (N6-adenosine-methyltransferase 70 kDa subunit) enzyme activity: X-Y-Z (I) wherein X, Y and Z are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, and autoimmune diseases, as well as other diseases or conditions in which METTL3 activity is implicated.
Synthetic method of 1, 7-naphthyridine derivative
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Paragraph 0039-0043; 0048-0052, (2020/03/29)
The invention discloses a synthetic method of a 1, 7-naphthyridine derivative, and relates to the technical field of synthesis of medical intermediates and organic chemical intermediates. The method comprises the following steps of: (1) taking 2-chloro-3-amino-pyridine as a compound I, taking the compound I as a starting raw material, and protecting amino to prepare a compound II; (2) reacting thecompound II with an hydroformylation reagent under an alkaline condition to obtain a compound III; and (3) carrying out cyclization reaction on the compound III and an acrylate compound under the action of Lewis acid to prepare a compound IV. The synthetic method disclosed by the invention is suitable for industrial production, relatively low in cost and simple to operate.
SMALL MOLECULE INHIBITORS OF NF-kB INDUCING KINASE
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Page/Page column 155, (2020/12/11)
The present invention relates to compounds that inhibit NIK and pharmaceutical compositions comprising such compounds and methods of using the same. These compounds and pharmaceutical compositions are envisaged to be useful for preventing or treating diseases such as cancer (such as B-cell malignancies including leukemias, lymphomas and myeloma), inflammatory disorders, autoimmune disorders, immunodermatologic disorders such as palmoplantar pustulosis and hidradenitis suppurativa, and metabolic disorders such as obesity and diabetes.
HYDROXYL PURINE COMPOUNDS AND USE THEREOF
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Paragraph 0570; 0571, (2018/04/05)
Disclosed are a series of hydroxyl purine compounds and the use thereof as PDE2 or TNFα inhibitors, in particular, the compounds as shown in formula (I), or tautomers thereof or pharmaceutically acceptable salts thereof.
HYDROXYL PURINE COMPOUNDS AND USE THEREOF
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Paragraph 0312; 0313, (2018/06/09)
Disclosed are a series of hydroxyl purine compounds and the use thereof as PDE2 or TNFα inhibitors, in particular, the compounds as shown in formula (I), or tautomers or pharmaceutically acceptable salts thereof.
Ligand-Promoted Meta-C-H Arylation of Anilines, Phenols, and Heterocycles
Wang, Peng,Farmer, Marcus E.,Huo, Xing,Jain, Pankaj,Shen, Peng-Xiang,Ishoey, Mette,Bradner, James E.,Wisniewski, Steven R.,Eastgate, Martin D.,Yu, Jin-Quan
supporting information, p. 9269 - 9276 (2016/08/05)
Here we report the development of a versatile 3-acetylamino-2-hydroxypyridine class of ligands that promote meta-C-H arylation of anilines, heterocyclic aromatic amines, phenols, and 2-benzyl heterocycles using norbornene as a transient mediator. More than 120 examples are presented, demonstrating this ligand scaffold enables a wide substrate and coupling partner scope. Meta-C-H arylation with heterocyclic aryl iodides as coupling partners is also realized for the first time using this ligand. The utility for this transformation for drug discovery is showcased by allowing the meta-C-H arylation of a lenalidomide derivative. The first steps toward a silver-free protocol for this reaction are also demonstrated.
Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors
Demont, Emmanuel H.,Chung, Chun-Wa,Furze, Rebecca C.,Grandi, Paola,Michon, Anne-Marie,Wellaway, Chris,Barrett, Nathalie,Bridges, Angela M.,Craggs, Peter D.,Diallo, Hawa,Dixon, David P.,Douault, Clement,Emmons, Amanda J.,Jones, Emma J.,Karamshi, Bhumika V.,Locke, Kelly,Mitchell, Darren J.,Mouzon, Bernadette H.,Prinjha, Rab K.,Roberts, Andy D.,Sheppard, Robert J.,Watson, Robert J.,Bamborough, Paul
, p. 5649 - 5673 (2015/08/03)
Overexpression of ATAD2 (ATPase family, AAA domain containing 2) has been linked to disease severity and progression in a wide range of cancers, and is implicated in the regulation of several drivers of cancer growth. Little is known of the dependence of
CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
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Paragraph 0262, (2015/03/13)
Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described.
Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors
Labadie, Sharada,Barrett, Kathy,Blair, Wade S.,Chang, Christine,Deshmukh, Gauri,Eigenbrot, Charles,Gibbons, Paul,Johnson, Adam,Kenny, Jane R.,Kohli, Pawan Bir,Liimatta, Marya,Lupardus, Patrick J.,Shia, Steven,Steffek, Micah,Ubhayakar, Savita,Abbema, Anne Van,Zak, Mark
, p. 5923 - 5930 (2013/10/22)
A highly ligand efficient, novel 8-oxo-pyridopyrimidine containing inhibitor of Jak1 and Jak2 isoforms with a pyridone moiety as the hinge-binding motif was discovered. Structure-based design strategies were applied to significantly improve enzyme potency and the polarity of the molecule was adjusted to gain cellular activity. The crystal structures of two representative inhibitors bound to Jak1 were obtained to enable SAR exploration.