349395-87-5Relevant academic research and scientific papers
Derivatives with uracil-benzothiazole structure, preparation method of derivatives, and application of anti-HCV drugs
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Paragraph 0067-0069, (2019/12/02)
According to the invention, a new series of uracil-benzothiazole NS5B RdRp inhibitors are designed and synthesized; the compounds have the structure shown in a general formula (1), wherein the uracil-benzothiazole NS5B RdRp inhibitor provided by the inven
Derisking the Cu-Mediated 18F-Fluorination of Heterocyclic Positron Emission Tomography Radioligands
Taylor, Nicholas J.,Emer, Enrico,Preshlock, Sean,Schedler, Michael,Tredwell, Matthew,Verhoog, Stefan,Mercier, Joel,Genicot, Christophe,Gouverneur, Véronique
supporting information, p. 8267 - 8276 (2017/06/27)
Molecules labeled with fluorine-18 (18F) are used in positron emission tomography to visualize, characterize and measure biological processes in the body. Despite recent advances in the incorporation of 18F onto arenes, the development of general and efficient approaches to label radioligands necessary for drug discovery programs remains a significant task. This full account describes a derisking approach toward the radiosynthesis of heterocyclic positron emission tomography (PET) radioligands using the copper-mediated 18F-fluorination of aryl boron reagents with 18F-fluoride as a model reaction. This approach is based on a study examining how the presence of heterocycles commonly used in drug development affects the efficiency of 18F-fluorination for a representative aryl boron reagent, and on the labeling of more than 50 (hetero)aryl boronic esters. This set of data allows for the application of this derisking strategy to the successful radiosynthesis of seven structurally complex pharmaceutically relevant heterocycle-containing molecules.
Modification of a dihydropyrrolopyrimidine phosphoinositide 3-kinase (PI3K) inhibitor to improve oral bioavailability
Kawada, Hatsuo,Ebiike, Hirosato,Tsukazaki, Masao,Yamamoto, Shun,Koyama, Kohei,Nakamura, Mitsuaki,Morikami, Kenji,Yoshinari, Kiyoshi,Yoshida, Miyuki,Ogawa, Kotaro,Shinma, Nobuo,Tsukuda, Takuo,Ohwada, Jun
, p. 7650 - 7660 (2015/12/18)
Phosphoinositide 3-kinase (PI3K) is activated in various human cancer cells and well known as a cancer therapy target. We previously reported a dihydropyrrolopyrimidine derivative as a highly potent PI3K inhibitor that has strong tumor growth inhibition in a xenograft model. In this report, we describe further optimization to improve its bioavailability.
Discovery of novel potent and highly selective glycogen synthase kinase-3β (GSK3β) inhibitors for Alzheimers Disease: Design, synthesis, and characterization of pyrazines
Berg, Stefan,Bergh, Margareta,Hellberg, Sven,Hoegdin, Katharina,Lo-Alfredsson, Yvonne,Soederman, Peter,Von Berg, Stefan,Weigelt, Tatjana,Ormoe, Mats,Xue, Yafeng,Tucker, Julie,Neelissen, Jan,Jerning, Eva,Nilsson, Yvonne,Bhat, Ratan
, p. 9107 - 9119,13 (2020/10/15)
Glycogen synthase kinase-3β, also called tau phosphorylating kinase, is a proline-directed serine/threonine kinase which was originally identified due to its role in glycogen metabolism. Active forms of GSK3β localize to pretangle pathology including dystrophic neuritis and neurofibrillary tangles in Alzheimers disease (AD) brain. By using a high throughput screening (HTS) approach to search for new chemical series and cocrystallization of key analogues to guide the optimization and synthesis of our pyrazine series, we have developed highly potent and selective inhibitors showing cellular efficacy and bloo-brain barrier penetrance. The inhibitors are suitable for in vivo efficacy testing and may serve as a new treatment strategy for Alzheimers disease.
INHIBITORS OF JANUS KINASES
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Page/Page column 40-41, (2010/04/03)
The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2). The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, J
AROMATIC COMPOUND
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Page/Page column 76-77, (2008/12/07)
An aromatic compound represented by the following formula or a pharmaceutically acceptable salt thereof: , wherein ring A is a heterocyclic ring, ring B is a carbocyclic ring, a heterocyclic ring etc., G1, G2, G3, G4 and G5 are CH or N, X is -NH-, -O-, -CH2-, etc., Y is - CH2-,-CO-,-SO2- etc., Z is a single bond, -CO-, -SO2-, -NH-, -O-, -S-, -CONH-,-SO2NH-, etc., R2 is hydrogen, alkyl, alkoxy, halogen, etc., and R3 is carbocyclic group, heterocyclic group, alkyl, etc., is useful as a controlling agent of the function of CCR4 useful for the treatment or therapy for bronchial asthma, atopic dermatitis, etc.
Benzotriazine inhibitors of kinases
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Page/Page column 106, (2008/06/13)
The invention provides benzotriazine compounds having formula (I). The benzotriazine compounds of the invention are capable of inhibiting kinases, such members of the Src kinase family, and various other specific receptor and non-receptor kinases.
