915019-53-3Relevant academic research and scientific papers
Development of a Robust Synthesis of Dactolisib on a Commercial Manufacturing Scale
Baenziger, Markus,Pachinger, Werner,Stauffer, Frédéric,Zaugg, Werner
, p. 1908 - 1917 (2019/09/30)
The development of the robust synthesis of 2-methyl-2-[4-[3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydro-1H-imidazo[4,5-c]quinolin-1-yl]-phenyl]propionitrile (dactolisib) on a commercial scale is described. The key step is a Pd-catalyzed Suzuki coupling of 2-[4-(8-bromo-3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinolin-1-yl)-phenyl]-2-methyl-propionitrile to 3-quinoline boronic acid. A special focus is placed on reducing the amount of Pd catalyst used in the Suzuki coupling and purifying the crude drug substance, including removing traces of Pd.
C26-LINKED RAPAMYCIN ANALOGS AS MTOR INHIBITORS
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, (2019/11/21)
The present disclosure relates to mTOR inhibitors. Specifically, the embodiments are directed to compounds and compositions inhibiting mTOR, methods of treating diseases mediated by mTOR, and methods of synthesizing these compounds.
RAPAMYCIN ANALOGS AS MTOR INHIBITORS
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, (2018/12/03)
The present disclosure relates to rapamycin analogs of the general Formula (I). The compounds are inhibitors of mTOR and thus useful for the treatment of cancer, immune-mediated diseases and age related conditions.
FUSED QUINOLINE COMPUNDS AS PI3K/MTOR INHIBITORS
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, (2017/02/09)
The present invention relates to the compounds of formula I, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states associated with cancers associated with protein kin
Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof
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, (2016/04/26)
The present invention provides for a method for treating a disease condition associated with PI3-kinase α and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase α and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth.
JAK PI3K/mTOR combination therapy
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, (2016/06/28)
Provided herein is a combination therapy comprising a JAK kinase inhibitor and a dual PI3K/mTOR inhibitor, as well as methods of treating various cancers through the use of such a combination therapy.
Imidazole derivatives, its pharmaceutical composition and use thereof
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, (2017/02/24)
Imidazolone compounds, pharmaceutically acceptable salts, solvates, polymorphs or prodrugs thereof are disclosed. Pharmaceutical compositions comprising above substances and uses for preventing and treating protein kinases related diseases, such as cancers, metabolic diseases, cardiovascular diseases and the like, are also disclosed.
COMBINATION OF KINASE INHIBITORS AND USES THEREOF
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, (2015/02/19)
The present invention provides for a method for treating a disease condition associated with PI3-kinase a and/or a receptor tyrosine kinase (RTK) in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase α and/or an RTK in a subject. In yet another aspect, a method of inhibiting phosphorylation of Akt (S473) in a cell is set forth.
HETEROCYCLIC COMPOUNDS AND USES THEREOF
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, (2015/11/30)
Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the heterocyclic entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.
COMBINATION OF KINASE INHIBITORS AND USES THEREOF
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, (2014/10/04)
The present invention provides for a method for treating a disease condition associated with PI3-kinase a and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase a and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth. The present invention also provides a pharmaceutical kit effective for treating a disease condition associated with PI3 -kinase α and/or mTOR in a subject.
