172324-68-4Relevant articles and documents
COMPOUNDS AND METHODS FOR TARGETED DEGRADATION OF KRAS
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Paragraph 00334, (2021/10/15)
Bifunctional compounds, which find utility as modulators of Kirsten ras sarcoma protein (KRas or KRAS), are described herein. In particular, the hetero-bifunctional compounds of the present disclosure contain on one end a moiety that binds to the Von Hippel-Lindau E3 ubiquitin ligase and on the other end a moiety which binds KRas, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The heterobifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
IRAK DEGRADERS AND USES THEREOF
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Paragraph 00920; 001251-001253; 002232, (2021/01/23)
The present invention provides compounds, compositions thereof, and methods of using the same. The compounds include an IRAK binding moiety capable of binding to IRAK4 and a degradation inducing moiety (DIM). The DIM could be DTM a ligase binding moiety (LBM) or lysine mimetic. The compounds could be useful as IRAK protein kinase inhibitors and applied to IRAK mediated disorders.
Synthesis and evaluation of 2′-substituted cyclobutyl nucleosides and nucleotides as potential anti-HIV agents
Li, Yongfeng,Mao, Shuli,Hager, Michael W.,Becnel, Kimberlynne D.,Schinazi, Raymond F.,Liotta, Dennis C.
, p. 3398 - 3401 (2008/02/09)
A series of 2′-substituted cyclobutyl nucleoside analogs were efficiently prepared by constructing the core cyclobutyl ring using different [2+2] cycloaddition approaches. The triphosphate derivative of a cyclobutyl nucleoside was also synthesized and eva
USE OF PDE7 INHIBITORS FOR THE TREATMENT OF NEUROPATHIC PAIN
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Page/Page column 78, (2008/06/13)
The present invention relates to the use of a phosphodiesterase 7 (PDE7) inhibitor in the manufacture of a medicament for the treatment of neuropathic pain and to a method of treating neuropathic pain using an inhibitor of PDE7.
Synthesis of 9--adenine and -guanine
Kaiwar, Vijay,Reese, Colin B.,Gray, Emily J.,Neidle, Stephen
, p. 2281 - 2288 (2007/10/02)
2,2-Dichloro-3-(benzyloxymethyl)cyclobutanone 15, which was prepared in 50percent yield by the cycloaddition of dichloroketene to allyl benzyl ether 14, was converted in four steps and in ca. 40percent overall yield into trans-3-(benzyloxymethyl)cyclobutanol 11b.The latter alcohol 11b was coupled under Mitsunobu conditions with 6-(4-chlorophenylsulfanyl)-9H-purine 21b and 6-(4-chlorophenylsulfanyl)-2-(phenylacetamido)-9H-purine 21c to give the 9-cyclobutylpurine derivatives 22 and 24, respectively, in 88 and 60percent yield.The former product 22 was converted in three steps and in 39percent overall yield into 9-adenine 6, and the latter product was converted in four steps and in 42percent overall yield into 9-guanine 7.X-Ray crystallographic data relating to compounds 22 and 24 are also reported.
