17228-63-6Relevant articles and documents
Target-Based Identification and Optimization of 5-Indazol-5-yl Pyridones as Toll-like Receptor 7 and 8 Antagonists Using a Biochemical TLR8 Antagonist Competition Assay
Knoepfel, Thomas,Nimsgern, Pierre,Jacquier, Sébastien,Bourrel, Marjorie,Vangrevelinghe, Eric,Glatthar, Ralf,Behnke, Dirk,Alper, Phil B.,Michellys, Pierre-Yves,Deane, Jonathan,Junt, Tobias,Zipfel, Géraldine,Limonta, Sarah,Hawtin, Stuart,Andre, Cedric,Boulay, Thomas,Loetscher, Pius,Faller, Michael,Blank, Jutta,Feifel, Roland,Betschart, Claudia
, p. 8276 - 8295 (2020)
Inappropriate activation of endosomal TLR7 and TLR8 occurs in several autoimmune diseases, in particular systemic lupus erythematosus (SLE). Herein, the development of a TLR8 antagonist competition assay and its application for hit generation of dual TLR7
NOVEL HETEROCYCLIC DERIVATIVES USEFUL AS SHP2 INHIBITORS
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Page/Page column 84, (2020/05/12)
Provided is a compound of formula I, their synthesis and their use for treating a SHP2 mediated disorder. More particularly, provided is a pharmaceutical composition comprising the said compound.
COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF SHP2
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Paragraph 00404, (2017/01/02)
The present invention relates to compounds of formula I. The compounds are inhibitors of the Src Homolgy-2 phosphatase (SHP2) and thus useful in the treatment of Noonan Syndrome, Leopard Syndrome and cancer.
INHIBITORS OF LYSINE SPECIFIC DEMETHYLASE-1
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Paragraph 00179, (2016/04/26)
The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
Iron-catalyzed regioselective direct arylation at the C-3 position of N-alkyl-2-pyridone
Modak, Atanu,Rana, Sujoy,Maiti, Debabrata
, p. 296 - 303 (2016/09/09)
A number of pharmaceutical compounds possess an arylated 2-pyridone moiety. The existing reports using expensive starting materials and/or superstoichiometric metal salts have prompted us to explore a possible user-friendly method for their synthesis. In this report, we demonstrate an easy-to-handle reaction condition with an iron catalyst for the exclusive generation of C-3-arylated pyridone via C-H functionalization.
BENZAMIDE DERIVATIVES AS P2X7 RECEPTOR ANTAGONISTS
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Paragraph 0734;0735, (2014/03/25)
The invention relates to benzamide derivatives of formula (I), wherein R1, R2, R3, R4, R5, R6, n and Y are as defined in the description, their preparation and their use as pharmaceutically active compounds.
BENZAMIDE DERIVATIVES AS P2X7 RECEPTOR ANTAGONISTS
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Page/Page column 101, (2012/09/11)
The invention relates to benzamide derivatives of formula (I),wherein R1, R2, R3, R4, R5, R6, n and Y are as defined in the description, their preparation and their use as pharmaceutically active compounds.
One-pot synthesis of benzo[f]quinolin-3-ones and benzo[a]phenanthridein-5- ones by the photoanuulation of 6-chloropyridin-2-ones and 3-chloroisoquinolin-1- ones to phenylacetylene
Wang, Ren,Lu, Shen-Ci,Zhang, Yi-Ming,Shi, Zong-Jun,Zhang, Wei
, p. 5802 - 5808 (2011/10/02)
The one-pot synthesis of benzo[f]quinolin-3-ones and benzo[a] phenanthridein-5-ones was achieved by the inter- and intramolecular photoannulation of 6-chloropyridin-2-ones and 3-chloroisoquinolin-1-ones with phenylacetylene or tethered phenylacetylene. The reactions were proceeded by photoaddition of 6-chloropyridin-2-ones and 3-chloroisoquinolin-1-ones to phenylacetylene to give the chlorine-substituted stilbenoids, and then 6π electrocyclization of the stilbenoids and oxidation aromatization to afford the polycyclic products.
QUINOLINE COMPOUNDS AND METHODS OF USE
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Page/Page column 126; 127, (2008/06/13)
Compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof, are useful for inhibiting receptor tyrosine kinases and for treating hyperproliferative disorders mediated thereby. Methods of using compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. [ Formula I]
Ergoline derivatives and their use as somatostatin receptor antagonists
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, (2008/06/13)
The invention provides compounds of formula I wherein R1to R6are as defined in the description, and a process for preparing them. The compounds of formula I are useful as pharmaceuticals.