259262-49-2Relevant academic research and scientific papers
TAU-PROTEIN TARGETING COMPOUNDS AND ASSOCIATED METHODS OF USE
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Paragraph 1456; 1457, (2021/02/12)
The present disclosure relates to bifunctional compounds, which find utility as modulators of tan protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tan protein, such that tan protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tan. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tan protein. Diseases or disorders that result from aggregation or accumulation of tan protein are treated or prevented with compounds and compositions of the present disclosure.
BICYCLIC INHIBITORS OF HISTONE DEACETYLASE
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Paragraph 00107, (2020/02/06)
Provided herein are compounds of Formula I and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with histone deacetylases (HDAC).
Alkyl aryl ether bond formation with phenofluor
Shen, Xiao,Neumann, Constanze N.,Kleinlein, Claudia,Goldberg, Nathaniel W.,Ritter, Tobias
supporting information, p. 5662 - 5665 (2015/05/27)
An alkyl aryl ether bond formation reaction between phenols and primary and secondary alcohols with PhenoFluor has been developed. The reaction features a broad substrate scope and tolerates many functional groups, and substrates that are challenging for more conventional ether bond forming processes may be coupled. A preliminary mechanistic study indicates reactivity distinct from conventional ether bond formation. From fluorination to etherification: A method for the formation of alkyl aryl ethers directly from the corresponding alcohols and phenols with PhenoFluor has been developed. The reaction features a broad substrate scope, and substrates that are challenging for more conventional ether bond forming processes may be coupled. TMS=trimethylsilyl.
Synthesis of aryloxyazetidine derivatives by CuI/l-proline catalyzed coupling reaction of arylboronic acid with 1-Boc-3-iodoazetidine
Song, Juanjuan,Li, Xinjian,Liang, Apeng,Li, Jingya,Zou, Dapeng,Wu, Yangjie,Wu, Yusheng
, p. 2369 - 2372 (2014/05/06)
A novel CuI/l-proline catalyzed coupling reaction of 1-Boc-3-iodoazetidine with various arylboronic acids which produced aryloxyazetidine derivatives in moderate to good yields was investigated.
PYRIDYL ETHERS AND THIOETHERS AS LIGANDS FOR NICOTINIC ACETYLCHOLINE RECEPTOR AND ITS THERAPEUTIC APPLICATION
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Page 6-7; 9, (2010/02/07)
The present invention provides compounds of the formula:wherein m is 0, 1 or 2; p is 0 or 1; Y is O, S, S(O) or S(O)2 and R1 to R7 are various substituents as selective modulators of the nicotinic acetylcholine receptor useful in the treatment of pain, Al
Pyridyl ethers and thioethers as ligands for nicotinic acetylcholine receptor and its therapeutic application
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, (2008/06/13)
The present invention provides compounds of the formula: wherein m is 0, 1 or 2; p is 0 or 1; Y is O, S, S(O) or S(O)2 and R1 to R7 are various substituents as selective modulators of the nicotinic acetylcholine receptor u
Synthesis and structure-activity relationship of novel pyridyl ethers for the nicotinic acetylcholine receptor
Lee, Jung,Davis, Coralie B.,Rivero, Ralph A.,Reitz, Allen B.,Shank, Richard P.
, p. 1063 - 1066 (2007/10/03)
The preparation of novel pyridyl ethers as ligands for the nicotinic acetylcholine receptor (nAChR) is described. Variations of the ring size of the azacycle and substitution on the pyridine had dramatic effects on receptor binding affinity with IC50S at the α4β2 nAChR ranging from 22 to >10,000 nM. The most potent molecule was (R)-2-chloro-3-(4-cyanophenyl)-5-((3-pyrrolidinyl)oxy)pyridine 27f with an IC50 of 22 nM. (C) 2000 Elsevier Science Ltd. All rights reserved.
