917887-34-4Relevant articles and documents
Novel CDK inhibitory compounds, preparation method thereof, pharmaceutical composition for use in preventing or treating CDK relating diseases containing the same as an active ingredient
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, (2018/10/24)
The present invention relates to a novel CDK inhibitory compound, a method for manufacturing the same, and a pharmaceutical composition for preventing or treating a CDK-related disease containing the compound as an active ingredient. The novel CDK inhibit
Investigations into the synthesis, radiofluorination and conjugation of a new [18F]fluorocyclobutyl prosthetic group and its in vitro stability using a tyrosine model system
Franck, Dominic,Kniess, Torsten,Steinbach, Joerg,Zitzmann-Kolbe, Sabine,Friebe, Matthias,Dinkelborg, Ludger M.,Graham, Keith
, p. 643 - 652 (2013/02/25)
The [18F]fluorocyclobutyl group has the potential to be a metabolically stable prosthetic group for PET tracers. The synthesis of the radiolabeling precursor cis-cyclobutane-1,3-diyl bis(toluene-4-sulfonate) 8 was obtained from epibromohydrin i
PRECURSOR COMPOUNDS AND METHODS FOR MAKING SAME
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, (2013/03/26)
The present invention relates to a method of obtaining radiopharmaceutical precursors, and in particular precursors to protected amino acid derivatives, which are used as precursors for production of radiolabelled amino acids for use in in vivo imaging procedures, such as positron emission tomography (PET).
Pre-steady state kinetic analysis of cyclobutyl derivatives of 2′-deoxyadenosine 5′-triphosphate as inhibitors of HIV-1 reverse transcriptase
Kim, Jiae,Wang, Ligong,Li, Yongfeng,Becnel, Kimberlynne D.,Frey, Kathleen M.,Garforth, Scott J.,Prasad, Vinayaka R.,Schinazi, Raymond F.,Liotta, Dennis C.,Anderson, Karen S.
supporting information; experimental part, p. 4064 - 4067 (2012/07/14)
Pre-steady state kinetic analysis was utilized for biochemical evaluation of a series of cyclobutyl adenosine nucleotide analogs with HIV-1 RT WT. The phosphonyl-diphosphate form of the cyclobutyl nucleotide, 5, was the most efficiently incorporated of the series. Nucleotide 5 was fourfold more efficiently incorporated than the FDA approved TFV-DP by RTWT. The kinetics of incorporation for 5 using the drug resistant mutant enzyme K65R was also determined. Compound 5 was threefold more efficiently incorporated compared to TFV-DP with RTK65R. These results demonstrate cyclobutyl adenosine analogs can act as substrates for incorporation by HIV-1 RT and be a potential scaffold for HIV inhibitors.
AZETIDINE AND CYCLOBUTANE DERIVATIVES AS JAK INHIBITORS
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Page/Page column 57-58, (2009/09/28)
The present invention relates to azetidine and cyclobutane derivatives, as well as their compositions, methods of use, and processes for preparation, which are JAK inhibitors useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.
A Versatile Synthesis of Four-, Five-, and Six-membered Cyclic Ketones Using Methyl Methylthiomethyl Sulfoxide
Ogura, K.,Yamashita, M.,Suzuki, M.,Furukawa, S.,Tsuchinashi, G.
, p. 1637 - 1642 (2007/10/02)
Cyclization of 1,n-dihaloalkanes with methyl methylthiomethyl sulfoxide in the presence of a base (n-BuLi or KH) gave three-, four-, five-, and six-membered 1-methylsulfinyl-1-methylthiocycloalkanes.These cyclization products were easily converted to the corresponding ketones by acid hydrolysis except 1-methylsulfinyl-1-methylthiocyclopropane which afforded a complicated mixture.The combination of the cyclization with the acidhydrolysis thus provides a new method for synthesizing four-, five-, and six-membered cycloalkanones.Several representative preparations, such as those of substituted cyclobutanones, 3-cyclopentanone, and tetrahydro-4-pyrone are described.
