915019-50-0Relevant 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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Paragraph 00441, (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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Paragraph 00336; 00337, (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.
Acid-Promoted Cascade Reaction of N-(4-Chloroquinolin-3-yl)carbamates with Amines: One-Pot Assembly of Imidazo[4,5-c]quinolin-2-ones
Lu, Xiao,Kim, Myunghoon,Orr, Meghan J.,Li, Hao,Huang, Wenwei
, p. 1572 - 1580 (2018/04/20)
An acid-promoted cascade reaction of N-(4-chloroquinolin-3-yl)carbamates with amines is described. This method achieves the formation of two new C–N bonds through an intermolecular amination/intramolecular cyclization reaction sequence. In combination wit
COMPOUNDS AND METHOD FOR BLOCKING TRANSMISSION OF MALARIAL PARASITE
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Paragraph 0073, (2018/04/27)
Disclosed are compounds of formula (I) and formula (II): (I) (II) wherein R1, R2, A, and B are as defined herein. Also disclosed is a method of blocking transmission of a Plasmodium parasite and a method of treating or preventing mal
Imidazole derivatives, its pharmaceutical composition and use thereof
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Paragraph 0210-0211, (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.
JAK PI3K/mTOR combination therapy
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Page/Page column 21, (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.
JAK P13K/mTOR COMBINATION THERAPY
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Page/Page column 30, (2013/03/26)
Provided herein is a combination therapy comprising a JAK kinase inhibitor and a dual PBK/mTOR inhibitor, as well as methods of treating various cancers through the use of such a combination therapy.
Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway
Stauffer, Frederic,Maira, Sauveur-Michel,Furet, Pascal,Garcia-Echeverria, Carlos
, p. 1027 - 1030 (2008/09/21)
Imidazo[4,5-c]quinoline derivatives have been discovered and developed as potent and effective modulators of the phosphatidylinositol 3-kinase (PI3K)/protein kinase B (PKB) pathway to lead to clinical development candidates. The SAR data of representative examples of this compound class and their biological profiling in cellular and in vivo settings are presented and discussed.
SALTS AND CRYSTALL FORMS OF 2-METHYL-2-[4-(3-METHYL-2-OXO-8-QUINOLIN-3-YL-2,3-DIHYDRO-IMIDAZO[4,5-C]QUINOLIN-1-YL)-PHENYL]-PROPIONITRILE
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Page/Page column 20, (2008/12/05)
The invention relates to particular crystalline forms of 2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile, its hydrates and solvates, its salts and hydrates and solvates of its salts, certain processes for their preparation, pharmaceutical compositions containing these crystalline forms, and their use in diagnostic methods or, preferably, for the therapeutic treatment of warm-blooded animals, especially humans, and their use as an intermediate or for the preparation of pharmaceutical preparations for use in diagnostic methods or, preferably, for the therapeutic treatment of warm-blooded animals, especially humans.
