690636-28-3Relevant academic research and scientific papers
Synthesis method of tirbanibulin intermediate
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Paragraph 0028-0033; 0036-0042, (2022/01/10)
The invention belongs to the technical field of synthesis of medical compounds, and particularly discloses a synthesis method of a tirbanibulin intermediate. According to the method, 4-[2-(4-bromophenoxy)ethyl]morpholine is adopted as a raw material, firstly reacts with an n-butyl magnesium lithium reagent and then reacts with isopropyl alcohol pinacol borate, and the tirbanibulin intermediate is synthesized through a one-pot method. The method is mild in reaction condition and simple to operate, the reaction product is single, the target product can be obtained at high yield through a simple post-treatment and recrystallization method, and the method is expected to be developed into an industrial production method.
BET INHIBITORS FOR MODULATING DUX4 EXPRESSION IN FSHD
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Page/Page column 94; 95, (2020/07/14)
The present disclosure provides BET inhibitors of the formula: wherein the variables are defined herein, as well as pharmaceutical compositions thereof. The present disclosure also provides methods of treating a patient comprising administering a bromo- and extra-terminal (BET) domain inhibitor for the treatment of FSHD which modulates DUX4 expression. In some embodiments, the present methods comprise using one or more BET inhibitors as a therapeutic agent for the treatment of FSHD patients including patients who are being treated with one or more palliative treatments such as therapy and/or agents which lead to increased muscle mass.
IN-FLOW PHOTOOXYGENATION OF AMINOTHIENOPYRIDINONES GENERATES NOVEL PTP4A3 PHOSPHATASE INHIBITORS
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Paragraph 00110, (2020/06/05)
The disclosure provides compounds that inhibit protein tyrosine phosphatase, such as protein tyrosine phosphatase 4A3 (PTP4A3). The disclosure also provides pharmaceutical compositions, uses, and methods of using the compounds, such as in the treatment of cancers. (I), wherein X is O or NH.
NOVEL HETEROAROMATIC COMPOUNDS AS POTENT MODULATORS OF THE HIPPO-YAP SIGNALING PATHWAY LATS1/2 KINASES
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Page/Page column 33, (2020/03/23)
The present invention relates to novel heteroaromatic compounds of formulae (I) and (II) and pharmaceutically acceptable salts thereof. The compounds of the invention are useful as inhibitors of serine/threonine protein kinases LATS1 and LATS2. Also provided herein are processes for making compounds of formulae (I) and (II), and pharmaceutical compositions comprising the compounds of the invention. The present invention also provides methods of treating cancer with a compound of formula (I) or (II).
In-flow photooxygenation of aminothienopyridinones generates iminopyridinedione PTP4A3 phosphatase inhibitors
Tasker, Nikhil R.,Rastelli, Ettore J.,Blanco, Isabella K.,Burnett, James C.,Sharlow, Elizabeth R.,Lazo, John S.,Wipf, Peter
supporting information, p. 2448 - 2466 (2019/03/06)
A continuous flow photooxygenation of 7-aminothieno[3,2-c]pyridin-4(5H)-ones to produce 7-iminothieno[3,2-c]pyridine-4,6(5H,7H)-diones has been developed, utilizing ambient air as the sole reactant. N-H Imines are formed as the major products, and excellent functional group tolerance and conversion on gram-scale without the need for chromatographic purification allow for facile late-stage diversification of the aminothienopyridinone scaffold. Several analogs exhibit potent in vitro inhibition of the cancer-associated protein tyrosine phosphatase PTP4A3, and the SAR supports an exploratory docking model.
Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361)
Smolinski, Michael P.,Bu, Yahao,Clements, James,Gelman, Irwin H.,Hegab, Taher,Cutler, David L.,Fang, Jane W. S.,Fetterly, Gerald,Kwan, Rudolf,Barnett, Allen,Lau, Johnson Y. N.,Hangauer, David G.
supporting information, p. 4704 - 4719 (2018/06/20)
The discovery of potent, peptide site directed, tyrosine kinase inhibitors has remained an elusive goal. Herein we describe the discovery of two such clinical candidates that inhibit the tyrosine kinase Src. Compound 1 is a phase 3 clinical trial candidat
Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan
Wang, Aoli,Li, Xixiang,Chen, Cheng,Wu, Hong,Qi, Ziping,Hu, Chen,Yu, Kailin,Wu, Jiaxin,Liu, Juan,Liu, Xiaochuan,Hu, Zhenquan,Wang, Wei,Wang, Wenliang,Wang, Wenchao,Wang, Li,Wang, Beilei,Liu, Qingwang,Li, Lili,Ge, Jian,Ren, Tao,Zhang, Shanchun,Xia, Ruixiang,Liu, Jing,Liu, Qingsong
, p. 8407 - 8424 (2017/11/03)
FLT3-ITD mutant has been observed in about 30% of AML patients and extensively studied as a drug discovery target. On the basis of our previous study that ibrutinib (9) exhibited selective and moderate inhibitory activity against FLT3-ITD positive AML cel
FLT3 kinase novel inhibitors and use thereof (by machine translation)
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Paragraph 0153; 0156; 0157, (2018/01/05)
The present invention provides FLT3 kinase novel inhibitors, of formula (I) compound or its pharmaceutically acceptable salt, solvate, isomer, ester, acid, metabolite, or prodrug. The invention also provides formula (I) compound of the pharmaceutical comp
ANTIVIRAL COMPOUNDS
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Page/Page column 440, (2014/09/29)
The present invention discloses compounds of Formula I: wherein the variables in Formula I are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formula I in the prevention or treatment of HCV infection.
NOVEL HYDROXAMIC ACID DERIVATIVE
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Paragraph 0358, (2013/03/26)
Provided is a novel compound which is useful as a pharmaceutical composition by inhibiting an LpxC activity, thereby exhibiting potent antimicrobial activity against gram-negative bacteria including Pseudomonas aeruginosa and its drug resistant bacteria. Provided is a hydroxamic acid derivative represented by the following general formula [1] or a pharmaceutically acceptable salt thereof:
