58584-92-2Relevant academic research and scientific papers
HETEROCYCLIC COMPOUNDS AS MTOR INHIBITORS
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Page/Page column 23-24, (2021/07/02)
The present disclosure describes novel heterocyclic mTOR inhibitors and methods for preparing them. The pharmaceutical compositions comprising such mTOR inhibitors and methods of using them for treating cancer, infectious diseases, and other mTOR associated disorders are also described.
PYRIDOPYRIMIDINE COMPOUNDS ACTING AS MTORC 1/2 DOUBLE-KINASE INHIBITORS
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Paragraph 0088-0091, (2020/11/30)
Disclosed are a series of pyridopyrimidine compounds and a use of same in the preparation of drugs associated with mTORC 1/2 dual complex inhibitors, and specifically disclosed is a use of the compounds as shown in formula (IV), tautomers thereof or pharmaceutically acceptable salts thereof in the preparation of drugs associated with mTORC 1/2 dual complex inhibitors.
HETEROARYL COMPOUNDS AND THEIR USE AS THERAPEUTIC DRUGS
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Paragraph 2308-2314, (2017/03/21)
The present invention provides heterocyclic compounds, the stereoisomer thereof, the enantiomer thereof, or the pharmaceutically acceptable salt, which are capable of modulating the activity of Mer receptor tyrosine kinase (MERTK). This invention also provides pharmaceutical compositions thereof, methods to prepare the said compounds, and the use of such compounds as a medicament. The present invention is directed to MERTK inhibitory compounds with marked potency, thereby having an outstanding potential for a pharmaceutical intervention of cancer and any other diseases related to MERTK dysregulation.
BENZOXAZINONE DERIVATIVES AND ANALOGUES THEREOF AS MODULATORS OF TNF ACTIVITY
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Page/Page column 65, (2016/12/26)
A series of substituted 3,4-dihydro-2H-.1,4-benzoxazin-3-one derivatives, and analogues thereof, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune
Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: The discovery of AZD8055 and AZD2014
Pike, Kurt G.,Malagu, Karine,Hummersone, Marc G.,Menear, Keith A.,Duggan, Heather M.E.,Gomez, Sylvie,Martin, Niall M.B.,Ruston, Linette,Pass, Sarah L.,Pass, Martin
, p. 1212 - 1216 (2013/03/14)
The optimization of a potent and highly selective series of dual mTORC1 and mTORC2 inhibitors is described. An initial focus on improving cellular potency whilst maintaining or improving other key parameters, such as aqueous solubility and margins over hERG IC50, led to the discovery of the clinical candidate AZD8055 (14). Further optimization, particularly aimed at reducing the rate of metabolism in human hepatocyte incubations, resulted in the discovery of the clinical candidate AZD2014 (21).
Synthesis and properties of 5-cyano-substituted nucleoside analog with a donor-donor-acceptor hydrogen-bonding pattern
Kim, Hyo-Joong,Chen, Fei,Benner, Steven A.
experimental part, p. 3664 - 3669 (2012/06/04)
6-Aminopyridin-2-ones form Watson-Crick pairs with complementary purine analogues to add a third nucleobase pair to DNA and RNA, if an electron-withdrawing group at position 5 slows oxidation and epimerization. In previous work with a nucleoside analogue trivially named dZ, the electron withdrawing unit was a nitro group. Here, we describe an analogue of dZ (cyano-dZ) having a cyano group instead of a nitro group, including its synthesis, pKa, rates of acid-catalyzed epimerization, and enzymatic incorporation.
NICOTINAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
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Page/Page column 14, (2010/09/07)
The disclosure relates to compounds of formula (I): wherein A, Z, Z′, L, R2 and R3 are as defined in the disclosure, to compositions comprising said compounds, and to methods for the manufacture and therapeutic use thereof.
HETEROCYCLIC JAK KINASE INHIBITORS
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Page/Page column 98, (2010/04/27)
The present invention relates to compounds of Formula (I) and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds provide a treatment for myeloproliferative disorders and cancer
COMPOSITION FOR AGRICULTURAL USE FOR CONTROLLING OR PREVENTING PLANT DISEASES CAUSED BY PLANT PATHOGENS
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Page/Page column 269, (2010/11/19)
Disclosed is a composition for agricultural use, which is used for controlling or preventing plant diseases caused by plant pathogens. The composition for agricultural use contains a compound represented by formula (1), a salt thereof or a hydrate of the compound or the salt. (1) [In the formula, Z represents an oxygen atom, a sulfur atom or NRz; and E represents a furyl group, a thienyl group, a pyrrolyl group, a tetrazolyl group, a thiazolyl group, a pyrazolyl group, a phenyl group or the like.]
COMBINATION 059
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, (2009/04/24)
This invention relates to a combination product, as defined herein, comprising a MEK inhibitor and a mTOR-selective inhibitor, and to methods for the production of an anti-cancer effect in a patient, which is accordingly useful in the treatment of cancer in a patient. More specifically the present invention relates to; a combination product, as defined herein, comprising a MEK inhibitor and a mTOR-selective inhibitor; a combination product, as defined herein, comprising a kit of parts comprising a MEK inhibitor and a mTOR-selective inhibitor; use of the combination product, as defined herein, in the treatment of cancer; a method of treating cancer comprising administering the combination product, as defined herein, to a patient. The combination product, as defined herein, and methods of the invention are also useful in the treatment of other diseases associated with the activity of MEK, and/or mTOR.
